Prodrug and Antedrug: Two Diametrical Approaches in Designing Safer Drugs |
Lee, Henry-J.
(College of Pharmacy and Pharmaceutical Science, Florida A&M University. Tallahassee, 32307, Florida, USA)
Cooperwood, John-S. (College of Pharmacy and Pharmaceutical Science, Florida A&M University. Tallahassee, 32307, Florida, USA) You, Zhengqing (College of Pharmacy and Pharmaceutical Science, Florida A&M University. Tallahassee, 32307, Florida, USA) Ko, Dong-Hoon (College of Pharmacy and Pharmaceutical Science, Florida A&M University. Tallahassee, 32307, Florida, USA) |
1 | Beaucamp, L. M., Orr, G. F., de Miranda, P., Burnette, T., Krenitsky, T. A., Amino Acid Ester Prodrugs of Acyclovir. Antiviral Chem. Chemother., 3, 157-164 (1992) DOI |
2 | Balzarini, J., Naesens, L., Slachmuylders, J., Niphuis, H., Rosenburg, I., Holy, A., Schellekens, H., De Clerq, E, 9-(2Phosphonylmehtoxyethyl) adenine (PMEA) Effectively Inhibits Retrovirus Replication In Vitro and Simian Immunodeficiency Virus Infection in Rhesus Monkeys. AIDS, 5, 21-28 (1991) PUBMED |
3 | Shama, S. K., Bagshawe, K. D., Springer, C. J., Burke, P. J., Rogers, G. T, Boden, J. A, Antcniw, P., Melton, R. G. and Sherwood, R. F., Antibody directed enzyme prodrug therapy (ADEPT): a three phase system. Dis. Marker, 9, 225-231 (1991) |
4 | Vrudhula, V. M., Svensson, H. P., Kennedy, K. A., Senter, P. D. and Wallace, P. M., Antitumor activities of a cepnalosporin prodrug combination with monoclonal antibody-b-lactamase conjugates. Bioconjug. Chem., 4,334-340 (1993) DOI ScienceOn |
5 | Biggadike, K., Angell, R. M., Burgess, C. M., Farrell, R. M., Hancock, A. P, Harker, A. J., Irving, W. R., Ioannou, C., Procopiou, P.A., Shaw, R. E., Solanke, Y. E., Singh, O. M. P., Snowden, M. A, Stubbs, R. J., Walton, S. and Weston, H. E, Selective plasma hydrolysis of glucocorticoid g-lactones and cyclic carbonates by the enzyme paraoxonase: an ideal plasma inactivation mechanism. J. Med. Chem., 43, 19-21 (2000) DOI ScienceOn |
6 | Freeman, S. M., Ramesh, Rand Marrogi, A. J., Immune system in suicide gene therapy. Lancet, 349, 2-3 (1997) DOI ScienceOn |
7 | Manouilov, K. K., Fedorov, I. I., Boudinot, F. D., White, C. A., Kotra, K. P., Schinazi, R. F., Hong, C. I., Chu, C. K., Lymphatic Targeting of Anti-HIV Nucleosides: Distribution of 3-Azido-3-Deoxythymidine (AZT) and 3-Azido-2,3-Deoxyuridine (AzdU) after Administration of Dipalmitoylpho-sphatidyl Prodrugs to Mice. Antiviral Chem. Chemother., 6, 230-238 (1995) DOI |
8 | McGuigan, C., Camarasa, M.J., Egberink, H., Hartmann, K., Karlsson, A, Perno, C. F., Balzarini, J., Design, synthesis and biological evaluation of novel nucleotide prod rugs as inhibitors of HIV replication. Int. Antiviral News, 5, 19-21 (1997a) |
9 | Aghi, M., Kramm, C. M., Chou, T. C., Breakefield, X. O. and Chiocca, E. A., Synergistic anticancer effects of ganciclovir/thymidine kinase and 5-fluorocytosine deaminase gene therapies. J. Natl. Cancer Inst., 90, 370-380 (1998) DOI ScienceOn |
10 | Balzarini, J., Karlsson, A., Aquaro, S., Perno, C.F., Cahard, D., Naesens, L., De Clercq, E., McGuigan, C., Mechanism of anti-HIV action of masked alaninyl d4T-MP derivatives. Proc, Natl. Acad. Sci. USA, 93, 7295-7299 (1996a) DOI ScienceOn |
11 | Bloch, A., Robins, M. J., McCarthy, J. R., Jr., The role of the 5Hydroxyl Group of Adenosine in Determining Substrate Specificity for Adenosine Deaminase. J. Med. Chem., 10, 908-912 (1967) DOI PUBMED |
12 | Boyd, M. R., Bacon, T. H., Sutton, D., Comparative Activity of Penciclovir and Acyclovir in Mice Infected Intraperitoneally with Herpes Simplex Virus Type 1 SC 16. Antimicrob. Agents Chemother., 37, 642-645 (1993) DOI PUBMED ScienceOn |
13 | Erhardt, P.W., Woo, C. M., Gorzynski, R. J. and Anclerson, W.G., Ultrashort-acting b-adrenergic blocking agent. 1. (Aryloxy)-propanolamines containing esters in the nitrogen substituent. J. Med. Chem., 25,1402-1407 (1982) DOI PUBMED |
14 | Culver, K. W., Ram, Z., Wallbridge, S., Ishii, H., Oldfield, E. H. and Blaese, R. M., In vivo gene transfer with retroviral vectorproducer cells for treatment of experimental brain tumors. Science, 256,1550-1552 (1992) DOI PUBMED |
15 | Dayer, P., Kubli, A, Kupfer, A, Courvoisier, F., Balant, L. and Fabre, J. Defective hydroxylation of bufuralol associated with side-effects of the drug in poor metabolizers. Br. J. Clin. Pharmacol., 12,750-751 (1982) |
16 | Elion, G. B., The biochemistry and mechanism of action of acyclovir. Antimicrob. Chemother., 12, Suppl. B:9-17 (1983) |
17 | Farquhar, D., Khan, S., Srivastva, D. N., Saunders, P. P., Synthesis and Antitumor Evaluation of Bis[(Pivaloyloxy) methyl]-2-Deoxy-5-Fluorouridine 5-Monophosphate (Fd-UMP): A Strategy to Introduce Nucleotides into Cells. J. Med. Chem., 37, 3902-3909 (1994) DOI ScienceOn |
18 | Freeman, S. M., Abboud, C. N., Whartenby, K. A., Packman, C. H., Koeplin, D. S., Moolten, F. L., Abraham, G. N., The 'bystander effect': tumor regression when a fraction of the tumor mass is genetically modified. Cancer Res., 53, 5274-5283 (1993) |
19 | Ge, K., Xu, L., Zheng, Z., Xu, D., Sun, L. and Liu, X., Transduction of cytosine deaminase gene makes rat glioma cells highly sensitive to 5-fluorocytosine. Int. J. Cancer, 71, 675-679 (1997) DOI ScienceOn |
20 | Hamamoto, U., Nakashima, H., Matsui, A., Matsuda, A, Ueda, T, Yamamoto, N., Inhibitory Effects of 2,3-Didehydro-2,3-Dideoxynucleosides on Infectivity, Cytopathic Effects and Replication of Human Immunodeficiency Virus. Antimicrob Agents Chemother., 31,908 (1987) |
21 | Kwon T., Heiman A. S., Oriaku E. T., Yoon K and Lee, H. J., New steroidal antiinflammatory antedrugs: steroidal [16a,17a-d]-3-carbethoxyisoxazolines. J. Med. Chem., 38, 1048-1051 (1995) DOI ScienceOn |
22 | Hong, C. I., Nechaev, A, West, C. R., Nucleoside Conjugates as Potential Antitumor Agents. 2. Synthesis and Biological Activity of 1-(b-D-Arabinofuranosyl)cytosine Conjugates of Prednisolone and Prednisone. J. Med. Chem., 22, 1428-1432 (1979a) DOI PUBMED |
23 | Jones, R. J., Arimilli, M. N., Lin, K.-Y., Louie, M. S., McGee, L. R., Shaw, J. -P., Burman, D., Lee, M., Kennedy, J. A., Prisbe, E. J., Bischofberger, N., Lee, W. A., Cundy, K. C., Abstract Op11; XII International Roundtable Nucleosides, Nucleotides and their biological Application, September 15-19, La Jolla, USA (1996) |
24 | Kodama, K., Morozumi, M., Saitoh, K., Kuninaka, A., Yoshino, H., Saneyoshi, M., Antitumor Activiy and Pharmacclogy of 1b-D-Arabinofuranosylcytosine-5-stearylphosphate: An Orally Active Derivative of 1-b-D-Arabinofuranosylcytosine. Jpn. J. Cancer Res., 80, 679 (1989) DOI PUBMED |
25 | Labaree, D. C., Reynolds, T. Y. and Hochberg, R. B., Estradiol-16a carboxylic acid esters as locally active estrogens. J. Med. Chem., 44,1802-1814 (2001) DOI ScienceOn |
26 | Lee, H. J., You, Z., Ko, D.-H. and McLean, H. M., Recent advances in prodrugs and antedrugs. Drug Discovery and Development, 1(2),235-244 (1998) |
27 | Lee, H. J., You, Z., Ko, D.-H. and Yoon, K. J., New steroidal anti-inflammatory agents: Prednisolone derivatives with an isoxazoline fusion at the 16- and 17-carbons and an alkyl carboxylate at the 16a-position. Drugs Exptl. Clin. Res., 24(2),57-66 (1998) |
28 | Lewis, L. D., Fowle, A. S. E., Bittiner, S. B., Human Gastrointestinal Absorption of Acyclovir from Tablet Duodenal Infusion and Sipped Solution. Br. J. Clin. Pharmacol., 21,459-462 (1986) DOI PUBMED ScienceOn |
29 | Lipworth, B. J., Systemic adverse effects of inhaled corticosteroid therapy: A systematic review and metaanalysis. Arch. Intern. Med., 159(9),941-955 (1999) DOI PUBMED ScienceOn |
30 | Lorey, M., Meier, C., De Clerq, E., Balzarini, J., New Synthesis and Antitumor Activity of CycloSal-Derivatives of 5-Fluoro-2-deoxyuridinemonophosphate. Nucleosides & Nucleotides, 16,789-792 (1997) DOI ScienceOn |
31 | Manouilov, K. K., Xu, Z. S., Boudinot, F. D., Schinazi, R. F. and Chu, C. K. Lymphatic Targeting of Anti-HIV Nucleosides: Distribution of 2,3-Dideoxyinosine after Intravenous and Oral Administration of Dipalmitoylphosphatidyl Prodrug in Mice. Antiviral Res., 34, 91-99 (1997) DOI ScienceOn |
32 | McGuigan, C., Cahard, D., Sheeka, H. M., De Clercq, E, Balzarini, J., Aryl Phosphoramidate Derivatives of d4T Have Improved Anti-HIV Efficacy in Tissue Culture and May Act by the Generation of a Novel Intracellular Metabolite. J. Med. Chem., 39,1748-1753 (1996) DOI ScienceOn |
33 | Meier, C., Knispel, T., De Clerq, E, Balzarini, J., ADA-Bypass by Lipophilic CycloSal-ddAMP Pro-nucleotides a Second Example of the Efficiency of the CycloSal-concept. Bioorg. Med. Chem. Lett., 7,1577-1582 (1997d) DOI ScienceOn |
34 | Meier, C., Knispel, T, De Clerq, E., Balzarini, J., CycloSal-pronucleotides of 2,3-Dideoxyadenosine and 2, 3-Dideoxy-2,3-didehydroadenosine: Synthesis and Antiviral Evaluation of a Highly Efficient Nucleotide Delivery System. J. Med. Chem., 42, 1604-1614 (1999a) DOI ScienceOn |
35 | Melton, R. G. and Sherwood, R. F., Antibody-enzyme conjugates for cancer therapy. Journal of the National Cancer Institute, 88,153 (1996) DOI PUBMED |
36 | Niculescu-Duvaz, I. and Springer, C. J., Development of prodrugs for ADEPT (antibody-directed prodrug therapy). Expert Opinion on Investigational Drugs. 3, 289 (1996) |
37 | Shama, S. K., Bagshawe, K. D., Burke, P. J., Boden, R. W. and Rogers, G. T., Inactivation and clearance of an anti-CEA carboxypeptidase G2 conjugate in blood after localization in a xenograft model. Br. J. Cancer, 61,659-662 (1990) DOI PUBMED ScienceOn |
38 | Palomino, E., Kessel, D., Horwitz, J. P., A Dihydropyridine Carriers System for Sustained Delivery of 2,3-Dideoxynucleosides to the Brain. J. Med. Chem., 32, 622 (1989) DOI PUBMED |
39 | Ram, Z., Culver, K. W., Oshiro, E. IV., Viola, J. J., Devroom, H. L., Otto, E., Long, Z., Chiang, Y. McGarrity, G. J., Muul, L. M., Katz, D., Blease, R.M. and Oldfield, E. H., Therapy of malignant brain tumors by intratumoral implantation of retroviral vector-producing cells. Nat. Med., 12, 1354-1361 (1997) |
40 | Rivera, G., Rhomes, J. A., Dahl, G. V., Pratt, C. B., Wood, A., Avery, T. L., Combined VM-26 and Cytosine Arabinoside in Treatment of Refractory Childhood Lymphocytic Leukemia. Cancer, 45, 1284 (1980) DOI PUBMED ScienceOn |
41 | Shama, S. K., Boden, J. A., Springer, C. J., Burke, P. J. and Bagshawe, K. D., Antibody-directed enzyme prodrug therapy (ADEPT). A three phase study in ovarian tumor xenografts. Cell. Biophys., 24, 219-228 (1994) PUBMED |
42 | Sherwood, R., Melton, R., Alwan, S. and Hughes, P., Purification and properties of carboxypeptidase G2 from Pseudomonas sp. strain RS-16. Use of a novel triazine dye affinity method. Eur. J. Biochem., 148,447-453 (1985) DOI ScienceOn |
43 | Siddiqui, A. Q., Ballatore, C., McGuigan, C., De Clerq, E, Balzarini, J., The Presence of Substituents on the Aryl Moiety of the Aryl Phosphoramidate Derivative of d4T Enhances Anti-HIV Efficacy in Cell Culture: A Structure-Activity Relationship. J. Med. Chem., 42, 393-399 (1999) DOI ScienceOn |
44 | Suzuki, T., Tada, H., Sato, E. and Tojima, Y., Examination on biological activities and fates of new steroids, steroid-17 -ylmethyl glycolates derivatives. Tohoku J. Exptl. Med., 187(2), 127-140 (1999b) DOI ScienceOn |
45 | Siemers, N. O., Kerr, D. E., Yarnold, S., Stebbins, M., Vrudhula, V. M., Hellstrom, I., Hellstrom, K. E. and Senter, P.D., Construction, expression, and activities of L49-sFv b-lactamase, a single-chain antibody fusion protein for anticancer prodrug activation. Bioconjug. Chem., 8, 510-519 (1997) DOI ScienceOn |
46 | Springer, C. J. and Niculescu-Duvaz, I., Gene-directed enzyme prodrug therapy (GDEPT): choice of prodrugs. Adv. Drug Deliv. Rev., 22, 351-364 (1996) DOI ScienceOn |
47 | Srinivas, R. V., Robbins, B. L., Connelly, M. C., Gong, Y-F., Bischofberger, N., Fridland, A., Metabolism and In Vitro Antiretroviral Activities of Bis(Pivaloyloxymethyl) Prodrugs of Acyclic Nucleoside Phosphonates. Antimicrob. Agents Chemother., 37, 2247-2250 (1993) DOI PUBMED ScienceOn |
48 | Torrence, P. F., Kinjo, J., Khamnei, S., Greig, N. H., Synthesis and Pharmacokinetics of a Dihydropyridine Chemical Delivery System for the Antiimmunodeficiency Virus Agent Dideoxycytidine. J. Med. Chem., 36, 529-537 (1993) DOI ScienceOn |
49 | Van Rompay, K. K. A., Cherrington, J. M., Marthas, M. L., Berardi, C. J., Mulato, A S., Spinner, A., Tarara, R. P., Canfield, D. R., Telm, S., Bischofberger, N., Pederson, N. C., 9-[2-(Phosphomethoxy)propyl]-adenine Therapy of Established Simian Immunodeficiency Virus Infection in Infant Rhe-sus Macaques. Antimicrob. Agents Chemother., 40, 2586-2591 (1996) PUBMED |
50 | Whitley, R. J., Gnann, J. W., Acyclovir: A Decade Later, N. Engl. J. Med., 327, 782-788 (1992) DOI PUBMED ScienceOn |
51 | Yoon, K.-J., Khalil, M. A., Kwon, T. Choi, S.-J. and Lee, H. J., Steroidal anti-inflammatory antedrugs: synthesis and pharmacological evaluation of 16a-alkoxycarbonyl-17-deoxyprednisolone derivatives. Steroids, 60, 445-451 (1995) DOI ScienceOn |
52 | Lee, H. J. and Ko, D.-H., A novel approach to the discovery of non-systemic anti-inflammatory steroids: Antedrug. Arch. Pharm. Res., 22(3), 279-287 (1999) DOI ScienceOn |
53 | Friend, D. R., Phillips, S. and Tozer, T.N., Colon-specific drug delivery from a glucoside prodrug in the guinea pig. Efficacy study. J. Control Release, 15, 47-54 (1991) DOI ScienceOn |
54 | Hong, C. I., Kirisitis, A. J., Buchheit, D. J., Nechaev, A., West, C. R., 1 b-D-Arabinofuranosylcytosine Conjugates of Thioether Phospholipids as a New Class of Potential Antitumor Drugs. Cancer Drug Delivery, 3, 101-113 (1986) DOI PUBMED ScienceOn |
55 | Juhasz, A and Bodor, N., Cardiovascular studies on different classes of soft drugs. Pharmazie., 55(3), 228-238 (2000) PUBMED |
56 | Procopiou, P. A., Biggadike, K., English, A. F., Farrell, R. M., Hagger, G. N., Hancock, A. P., Haase, M. V., lrvinq, W. R., Sareen, M., Snowden, M. A., Solanke, Y. E., Tralau-Stewart, C. J., Walton, S. and Wood, J. A., Novel glucocorticoid antedrugs possessing a 17b-(g-lactone) ring. J. Med. Chem., 44, 602-612 (2001) DOI ScienceOn |
57 | Shuto, S., Itoh, H., Obara, T., Nakagami, K., Yaso, M., Yaginuma, S., Tsujino, M., Saito, T New Neplanocin Analogues II. Enzymatic One-Step Synthesis and Antitumor Activity of 6-(3-sn-Phosphatidyl)Neplanocin a Derivatives. Nucleosides & Nucleotides, 11,437-446 (1992) DOI ScienceOn |
58 | Kanai, F., Lan, K. H., Shiratori, Y., Tanaka, T. Ohashi, M., Okudaira, T, Yoshida, Y., Wakimoto, H., Hamada, H., Nakabayashi, H., Tamaoki, T. and Omata, M., In vivo gene therapy for alpha-fetoprotein-producing hepatocellular carcinoma by adenovirus-mediated transfer of cytosine deaminase gene. Cancer Res., 57, 461-465 (1997) PUBMED |
59 | Ko, D.-H., Maponya, M. F., Khalil, M. A., Oriaku, E. T., You, Z. and Lee, H. J., New anti inflammatory steroids: [16a,17a-d]-isoxazoline derivatives of prednisolone and 9a-fluoroprednisolone. Med. Chem. Res., 7, 313-323 (1997) |
60 | Pue, M. A., Benet, L. Z., Pharmacokinetics of Fanciclovir in Man. Antiviral Chem. Chemother., 4 (Suppl. 1),47-55 (1993) DOI |
61 | Soliman, M. R. I. and Lee, H. J., Anti-inflammatory activity of acid ester derivatives of prednisolone. Res. Comm. Chem. Path. Pharm., 33(2), 357-360 (1981) |
62 | Stribbling, S. M., Friedlos, F., Martin, J., Davies, L., Spooner, R. A., Marais, R. and Springer, C. J., Regressions of established breast carcinoma xenografts by carboxypeptidase G2 suicide gene therapy and the prodrug CMDA are due to a bystander effect. Hm. Gene Ther., 11, 258-292 (2000) |
63 | Xie, H., Voronkov, M., Liotta, D. C., Korba, B. A., Schinazi, R. F., Richman, D. D., Hostetler, K. Y, Phosphatidyl-2, 3-dideoxy-3-thiacytidine: Synthesis and Antiviral Activity in Hepatitis Band HIV-1 Infected Cells. Antiviral Res., 28,113-120 (1995) DOI ScienceOn |
64 | You, Z., Khalil, M. A., Ko, D.-H. and Lee, H. J., Suppression of the Mattox rearrangement of 16a-cyanoprednisolones in acid: synthesis of methyl 16a-prednisolone carboxylates. Tetrahedron Lett., 36(19), 3303-3306 (1995) DOI ScienceOn |
65 | Girardet, J.L., Perigaud, C., Aubertin, A.M., Gosselin, G., Kim, A, Imbach, J.L., Bloorg. Med. Chem. Lett., 5, 2981-2984 (1995b) DOI ScienceOn |
66 | Starrett, J. E., Jr., Tortolani, D. R., Russel, J., Hitchcock, M. J. M., Whiterock, V., Martin, J. C., Mansuri, M. M., Synthesis, Oral Bioavailability Determination, and In Vitro Evaluation of Prodrugs of the Antiviral Agent 9-[2-(Phosphonomehtoxy)ethyl] adenine (PMEA). J. Med. Chem., 37, 1857-1864 (1994) DOI ScienceOn |
67 | Terrence, P. F., Kinjo, J.E., Lesiak, K., Balazarine, J., De Clerq, E, AIDS Dementia: Synthesis and Properties of a Derivative of 3-Azido-3-Deoxythymidine (AZT) That May Become Locked in the Central Nervous System. FEBS Lett., 234,135 (1988) DOI ScienceOn |
68 | Harnden, M. R., Jarvest, R. L., Bacon, T. H., Boyd, M. R., Synthesis and Antiviral Activity of 9-[4-Hydroxy-3(hydroxymethyl)but-1-yl]purines. J. Med. Chem., 30, 1636-1642 (1987) DOI PUBMED |
69 | Hong, C. I., Nechaev, A., Kirisits, A. J., Vig, R., West, C. R., Manouilov, K. K., Chu, C. K., Nucleoside Conjugates. 15. Synthesis and Biological Activity of Anti-HIV Nucleoside Conjugates of Ether and Thioether Phospholipids. J. Med. Chem., 39, 1771-1777 (1996) DOI ScienceOn |
70 | Shlipak, M. G., Simon, J. A., Vittinghoff, E., Lin, F., Barrett-Conner, E., Knopp, R. H., Levy, R. I. and Hulley, S. B., Estrogen and progestin, lipoprotein (a), and the risk of recurrent coronary heart disease events after menopause. JAMA, 283, 1845-1852 (2000) DOI ScienceOn |
71 | Hong, C. I., Nechaev, A., West, C. R, Nucleoside Conjugates as Potential Antitumor Agents. 2. Synthesis and Biological Activity of 1-(b-D-Arabinofuranosyl)cytosine Conjugates of Prednisolone and Prednisone. J. Med. Chem., 22, 1428-1432 (1979b) DOI PUBMED |
72 | Ji, F., Huang, F., Juhasz, A., Wu, Wand Bodor, N., Design, synthesis and evaluation of soft glycopyrrolate and its analog. Pharmazie., 55(3), 187-191 (2000) PUBMED |
73 | Lowenthal, R. M. and Eaton, K., Toxicity of chemotherapy. Dematol. Oncol. Clin. North Am., 10, 967-990 (1996) DOI ScienceOn |
74 | Nassens, L., Balazarini, J., De Clerq, E., Therapeutic potential of PMEA as an antiviral drug. Med. Virol., 4,147-159 (1993) DOI |
75 | Touraine, R. L., Vahanian, N., Ramsey and W. J., Blaese, R. M., Enhancement of the herpes simplex virus thymidine kinase ganciclovir bystander effect and its antitumor efficacy in vivo by pharmacologic manipulation of gap junctions. Hum. Gene Ther., 9, 2385-2391 (1998) DOI ScienceOn |
76 | Arimilli, M. N., Kim, C. U., Dougherty, J., Mulato, A., Oliyai, R, Shaw, J. P., Cundy, K. C., Bischofberger, N., Synthesis, In Vitro Biological Evaluation and Oral Bioavailability of 9-[2(Phosphonomethoxy)propyl]adenine (PMPA) Prodrugs. Antiviral Chem. Chemother., 8, 557-564 (1997) DOI |
77 | Avery, M. A. and Woolfrey, J. R., Antiinflammatory steroids. In Wolff, ME (Ed.), Medicinal Chemistry and Drug Discovery. John-Wiley&Sons, Inc. 281-376 (1997) |
78 | Bagshawe, K. D. and Begent, R. H. J., First clinical experience with ADEPT. Adv. Drug Delivery Rev., 22, 365-367 (1996) DOI ScienceOn |
79 | Sastry, J. K., Nehete, P. N., Khan, S., Nowak, B. J., Plunkett, W., Arlinghaus, R. B., Farquhar, D., Membrane-Permeable Dideoxyuridine 5-Monophosphate Analogue Inhibits Human Immunodeficiency Virus Infection. Mol. Pharmacol, 41, 441-445 (1992) PUBMED |
80 | Smythe, W. R., Hwang, H. C., Elshami, A. A., Amin, K. M., Eck, S. L., Davidson, B. L., Wilson, J. M., Kaiser, L. R. and Albelda, S. M., Treatment of experimental human mesothelioma using adenovirus transfer of the herpes simplex thymidine kinase gene. Ann. Surg., 222, 78-86 (1995) DOI PUBMED ScienceOn |
81 | Meier, C., Knispel, T, Marquez, V. E, Siddiqui, M. A, De Clerq, E, Balzarini, J., CycloSal-Pronucleotides of 2-Fluoro-araand 2-Fluoro-ribo-2,3-dideoxyadenosine as a Strategy to Bypass a Metabolic Blockade. J. Med. Chem., 42, 1615-1624 (1999b) DOI ScienceOn |
82 | Chu, C. K., Bhadti, V. S., Doshi, K. J., Etse, J. T., Gallo, J. M., Boudinot, F. D., Schinazi, R. F., Brain Targeting of Anti-HIV Nucleosides: Synthesis and In Vitro and In Vivo Studies of Dihydopyridine Derivatives of 3-Azido-2,3-dideoxyuridine and 3-Azido-3-deoxythymidine. J. Med. Chem., 33, 2188-2192 (1990) DOI PUBMED |
83 | Elshami, A. A., Saavedra, A., Zhang, H., Kucharczuk, J. C., Spray, D. C., Fishman, G. I., Amin, K. M., Kaiser, L. R. and Albeda S. M., Gap junctions playa role in the 'bystander effect' of the herpes simplex virus thymidine kinase ganciclovir system in vitro. Gene Ther., 3, 85-92 (1996) PUBMED |
84 | Freeman, S. M., McCune, C., Robinson, W., Abboud, C. N., Abraham, G. N., Angel, C. and Marrogi, A, The treatment of ovarian cancer with a gene modified cancer vaccine: a phase I study. Hum. Gene Ther., 6, 927-939 (1995) DOI ScienceOn |
85 | Peuch, F., Gosselin, G., Lefebvre, I., Pompon, A., Aubertin, A.M., Kirn, A, Imbach, J.L., Intracellular Delivery of Nucleoside Monophosphates Through a Reductase-Mediated Activation Process. Antiviral Res., 22, 155-174 (1993) DOI PUBMED ScienceOn |
86 | Hostetler, K. Y., Richman, D. D., Sridhar, C. N., Gardner, M. F., Antiviral Activity of Phosphatidyl-dideoxycytidine in Hepatitis B Infected Cells and Enhanced Hepatitic Uptake in Mice. Antiviral Res., 24, 59-67 (1994) DOI ScienceOn |
87 | Lee, H. J. and Soliman, M. R. I., Anti-inflammatory steroids without pituitary adrenal suppression. Science, 215, 989-991 (1982) DOI PUBMED |
88 | Tsai, C. C., Follis, K. E., Beck, T. W., Sabo, A., Bischofberger, N., Dailey, P. J., Effects of (R)-9-(2-Phosphonylmethoxypropyl) adenine Monotherapy on Chronic SIV Infection in Macaques. AIDS Research and Human Retroviruses, 13, 707-712 (1997) DOI ScienceOn |
89 | Balzarini, J., Wedgwood, O., Kruining, J., Pelemans, H., Heijtink, R., De Clercq, E, McGuigan, C., Anti-HIV and Anti-HBV Activity and Resistance Profile of 2, 3-Dideoxy-3-Thiacytidine (3TC) and Its Arylphosphoramidate Derivative CF 1109. Biochem. Biophys. Res. Comm., 225, 363-369 (1996c) DOI ScienceOn |
90 | Bodor, N. and Buchwald, P., Soft drug design: general principles and recent applications. Med. Res. Rev., 20(1), 58-101 (2000) DOI ScienceOn |
91 | Sharma, A. P., Ollapally, A. P., Lee, H. J., Synthesis and Anti-HIV Activity of Prodrugs of Azidothymidine. Antiviral Chem. Chemother., 4, 93-96 (1993) DOI |
92 | Meier, C., Knispel, T., Lorey, M., Balzarini, J., Cyclo-Sal-Pronucleotides: The Design and Biological Evaluation of a New Class of Lipophilic Nucleotide Prodrugs. Int. Antiviral News, 5, 183-186 (1997a) |
93 | Khalil, M. A., Kwon, T. and Lee, H. J., A novel approach to the development of safer anti inflammatory steroids: Antedrugs. Current Topics in Med. Chem., 1,173-202 (1993) |
94 | Ko, D.-H., Heiman, A. S., Hudson, C. E. and Lee, H. J., New steroidal antiinflammatory antedrugs: methyl 3,20-dioxo-9a-fluoro-11b,17a,21-trihydroxy-1 ,4-pregnadiene-16acarboxylate and its 21-O-acyl derivatives. Steroids, in the press (2001) |
95 | Kuriyama, S., Mitoro, A., Yamazaki, N., Tsujinoue, H., Nakatani, T, Akahane, T., Toyokawa, Y., Karma, H., Okamoto, S. and Fukui, H., Comparison of gene therapy with the herpes simplex virus thymidine kinase gene and the bacterial cytosine deaminase gene for the treatment of hepatocellular carcinoma. Scand. J. Gsstroenterol., 34,1033-1041 (1999) DOI ScienceOn |
96 | OMalley, B. W. Jr., Chen, S. H., Schwartz, M. R. and Woo, S. L., Adenovirus-mediated gene therapy for human head and neck squamous cell cancer in a nude mouse model. Cancer Res., 55, 1080-1085 (1995) PUBMED |
97 | Perigaud, C., Girardet, J.L., Lefebvre, I., Xie, M.Y., Aubertin, A.M., Kirn, A., Gosselin, G., Imbach, J.L., Sommadossi, J.P., Comparison of Cytotoxicity of Mononucleoside Phosphotriester Derivatives Bearing Biolabile Phosphate Protecting Groups in Normal Human Bone Marrow Progenitor Cells. Antiviral Chem. Chemother., 7, 338-345 (1996) DOI |
98 | Roche, E. B., Design of Biopharmaceutical Properties through Prodrugs and Analogs. Academy of Pharmaceutical Sciences Symposium, Washington DC (1977) |
99 | Caruso, M., Panis, Y, Gagandeep, S., Houssin, D., Salzmannn, J. L. and Klatzmann, D., Regression of established macroscopic liver metastases after in situ transduction of a suicide gene. Proc. Natl. Acad. Sci. USA, 90, 7024-7028 (1993) DOI ScienceOn |
100 | Heiman, A.S., Ko, D.-H., Chen, M. and Lee, H. J., New steroidal anti-inflammatory antedrugs: Methyl 3,20-dioxo-9a-fluoro-11 b,17a,21-trihydroxy-1 ,4-pregnadiene-16acarboxylate and methyl 21-acetyloxy-3,20-dioxo-11 b,17adihydroxy-9a-fluoro-1,4-pregnadiene-16a-carboxylate. Steroids, 62, 491-499 (1997) DOI ScienceOn |
101 | Pantaleo, G., Graziosi, C., Demarest, J. F., Butini, L., Montroni, M., Fox, C. H., Orenstein, J. M., Kotler, D. P., Fauci, A.S., HIV Infection is Active and Progressive in Lymphoid Tissue During the Clinical Latent Stage of Disease. Nature, 392, 355-358 (1993) |
102 | Tsai, C. C., Follis, K. E., Sabo, A., Beck, T. W. Grant, R. F., Bischofberger, N., Benveniste, R. E., Black, R., Prevention of SIV Infection in Macaques by (R)-9-(2-Phosphony-Imethoxypropyl) adenine. Science, 270, 1197-1199 (1995) DOI PUBMED ScienceOn |
103 | Valette, G., Pompon, A, Giradet, J.L., Gosselin, G., Periqaud, C., Gosselin, G., Imbach, J.L., Decomposition Pathways and in vitro HIV Inhibitory Effects of IsoddA Pronucleotides: Toward a Rational Approach for Intracellular Delivery of Nucleoside 5-Monophosphates. J. Med. Chem., 39, 1981-1990 (1996) DOI ScienceOn |
104 | Brouilette, G., Kawamura, M., Kumar, G. N. and Bodor, N., Soft drugs. 21. Design and evaluation of soft analogs of propantheline. J. Pharm. Sci. 85, 619 (1996) DOI ScienceOn |
105 | Bodor, N., Recent advances in retrometabolic drug design and targeting approaches. Pharmazie, 55(3), 163-166 (2000) PUBMED |
106 | Rolan, P., Pharmacokinetics of New Antiherpetic Agents. Clin. Pharmacokinet., 29, 333-340 (1995) DOI PUBMED ScienceOn |
107 | Walker, R. E., Vogel, S. E., Jaffe, H.S., Polis, M. A., Kovacs, J., Markowitz, N., Masur, H., Lane, H. C., A Phase I/II Study of PMEA in HIV Infected Patients. Abstracts of Papers; 1st National Conference on Human Retroviruses and Related Infections, Washington DC (1993) |
108 | Benzaria, S., Pelicano, H., Johnson, R., Maury, G., Imbach,J.L., Aubertin, AM., Obert, G., Gosselin, G., Synthesis, In Vitro Antiviral Evaluation, and Stability Studies of Bis(S-acyl2-thioethyl) Ester Derivatives of 9-[2-(Phosphonomethoxy)ethyl]adenine (PMEA) as Potential PMEA Prodrugs with Improved Oral Bioavailability. J. Med. Chem., 39, 4958-4965(1996). DOI ScienceOn |
109 | Bronson, J. J., Ghazzouli, I., Hitchcock, M. J. M., Russel, J. W., Klunk, L. J., Kern E. R., Martin, J. C., In vivo Anti-retrovirus and Anti-cytomegalovirus Activity of 9-((2-Phosphonylmethoxy)-ethyl)adenine (PMEA). Abstracts of Papers; 5th International Conference on AIDS, Montreal, Canada, Abstract M.C.P 74 (1989) |
110 | Domin, B. A, Mahony, W B. and Zimmerman, T P, Transport of 5-fluorouracil and uracil into human erythrocytes. Biochem. Pharmacol., 46, 503-510 (1993) DOI ScienceOn |
111 | De Miranda, P., Blum, M. R., Pharmacokinetics of Acyclovir After Intranvenous and Oral Administration. J. Antimicrob. Chemother., 12 (Suppl. B) 29-37 (1983) PUBMED |
112 | Huber, B. E., Austin, E. A., Richards, C. A., Davis, S. T. and Good, S. S., Metabolism of 5 fluorocytosine in human colorectal tumor cells transduced with the cytosine deaminase gene: significant antitumor effects when only a small percentage of tumor cells express cytosine deaminase. Proc. Natl. Acad. Sci. USA, 91,8302-8306 (1994) DOI ScienceOn |
113 | Klatzmann, D., Valery, C. A., Bensimon, G., Marro, B., Boyer, O., Mokhatari, K., Diquet, B., Salzmann, J. L. and Philippon, J., A phase 1/11 study of herpes simplex type 1 thymidine kinase 'suicide' gene therapy recurrent glioblastoma, Hum. Gene Ther., 9, 2595-2604 (1998) DOI ScienceOn |
114 | Melcher, A., Todryk, S., Hardwick, N., Ford, M., Jacobson, M. and Vile, R. G., Tumor immunogenicity is determined by the mechanism of cell death via induction of heat shock protein expression. Nat. Med., 4, 581-587 (1998) DOI ScienceOn |
115 | Suzuki, T., Sato, E., Tada, H. and Tojima, Y., Examination of local anti-inflammatory activities of new steroids, hemisuccinyl methyl glycolates. Biol. Pharm. Bull., 22(8), 816-821 (1999a) DOI PUBMED ScienceOn |
116 | Vere Hodge, R. A., Sutton, D., Boyd, M. R., Harnden, M. R., Jarvest, R. L., Selection of an Oral Prodrug (BRL 42810; Famciclovir) for the Antiherpesvirus Agent BRL 39123 [9-(4Hydroxy- 3-hydroxymethylbut-1-yl)guanine; Penciclovir]. Antimicrob. Agents Chemother., 33,1765-1773 (1989) DOI PUBMED ScienceOn |
117 | Hamamoto, U., Nakashima, H., Matsui, A., Matsuda, A., Ueda, T., Yamamoto, N., Inhibitory Effects of 2,3-Didehydro-2,3-Dideoxynucleosides on Infectivity, Cytopathic Effects and Replication of Human Immunodeficiency Virus. Antimicrob. Agents Chemother., 31, 908 (1987) |
118 | Hanna, N. N., Mauceri, H. J., Wayne, J. D., Hallahan, D. E., Kufe, D. Wand Weichselbaum, R. R., Viral directed cytosine deaminase/5-fluorocytosine gene therapy enhances radiation response in human cancer xenografts. Cancer Res., 57, 4205-4209 (1997) PUBMED |
119 | Ko, D.-H., Heima, A. S., Chen, M. and Lee, H. J., New steroidal anti-inflammatory antedrugs: methyl 21-desoxy-21-chloro-11b, 17a-dihydroxy-3,20-dioxo-1 ,4-pregnadiene-16acarboxylate, methyl 21-desoxy-21-chloro-11 b-hydroxy-3,20dioxo-1,4-pregnadiene-16a-carboxylate, and their 9a-fluoro derivatives. Steroids, 65, 210-218 (2000) DOI ScienceOn |
120 | Pandha, H. S., Martin, L. A., Rigg, A, Hurst, H. C., Stamp, G. W., Sikora, K. and Lemoine, N. R., J. Clin. Oncol., 17, 2180-2189 (1999) DOI PUBMED |
121 | Tokunaga, Y., Iwasa, T., Fujisaki, J., Sawai, S., Kagayama, A., Liposomal Sustained-Release Delivery Systems for Intravenouslnjection. III. AntitumorActivity of Lipophilic Mitomycin C Prodrug Bearing Liposomes. Chem. Pharm. Bull., 36,3565 (1988b) DOI PUBMED ScienceOn |
122 | Harnden, M. R., Jarvest, R. L., Boyd, M. R., Sutton, D., Vere Hodge, R. A., Prodrugs of the Selective Antiherpesvirus Agent 9-[4-Hydroxy-3-(hydroxymethyl)but-1-yl]guanine (BRL 39123) with Improved Gastrointestinal Absorption Properties. J. Med. Chem., 33,1765-1773 (1989a) |
123 | Bentires-Alj, M., Hellin, A. C. and Lechanteur, C., Cytosine deaminase suicide gene therapy for peritoneal carcinomatosis. Cancer Gene Ther., 7, 20-26 (2000) DOI ScienceOn |
124 | Filer, C. W., Allen, G. D., Brown, T. A., Metabolic and Pharmacokinetic Studies Following Oral Administration of 14C-Famciclovir to Healthy Subjects. Xenbiotica 24, 357-368 (1994) DOI ScienceOn |
125 | Ichikawa, T., Tamiya, T., Adachi, Y., Ono, Y., Matsumoto, K., Furuta, T., Yoshida, Y., Hamada, H. and Ohmato, T., In vivo efficacy and toxicity of 5-fluorocytosine/cytosine deaminase gene therapy for malignant gliomas mediated by adenovirus. Cancer Gene Ther., 7, 74-82 (2000) DOI ScienceOn |
126 | Kimura, T., Yamaguchi, T., Usuki, K., Kurosaki, Y., Nakayama, T., Fujiwara, Y., Matsuda, Y., Unno, K. and Suzuki, T., Colonic mucosa-specific pro-antedrugs for oral treatment of ulcerative colitis: design, synthesis and fate of methyl 20-glucopyranosyloxyprednisolonates. J. Control Release, 30, 125-135 (1994) DOI ScienceOn |
127 | Meier, C., De Clerq, E., Balzarini, J., Cyclo-Saligenyl-3-azido-2,3-dideoxythymidine monophosphate (CycioSal-AZTMP) A New Pro-nucleotide Approach. Nucleosides and Nucleotides, 16,793-796 (1997c) DOI ScienceOn |
128 | Balzarini, J., Egberink, H., Hartmann, K., Karlsson, A., Perno, C.F., Cahard, D., Naesens, L., Thormar, E., De Clercq, E., McGuigan, C., Mechanism of Anti-HIV Action of Masked Alaninyl 2,3-Dideoxy-2,3-Didehydrothymidine 5-Monophosphate Derivatives. Antiviral Res., 30, A18 (1996d) |
129 | De Clerq, E., Broad-spectrum anti-DNA virus and anti-retrovirus activity of phosphonylmethoxyalkylpurine and pyrimidines. Biochem. Pharmacol., 42, 963-972 (1991) DOI PUBMED ScienceOn |
130 | Geddes, D. M., Inhaled corticosteroids: Benefits and risks. Thorax, 47, 404-407 (1992) DOI PUBMED ScienceOn |
131 | Hortobagyi, G. N., Anthracyclines in the treatment of cancer: an overview. Drugs, 54,1-7 (1997) PUBMED |
132 | Hamilton, T. C. and Parkes, M. W., Bufuralol, a new betaadrenoceptor blocking agent in a series of benzofuran-2-ethanolamines. Part 2: Pharmacology. Arzneim.-Forsch. 27, 1410-1417 (1977) |
133 | Martin-du Pan, R. C., Vonlanthen, M. C. and Dubuis, J. M., Growth and collagen synthesis disorders in asthmatic children treated with inhaled steroids. Rev. Med., Suisse Romande, 119(6), 475-479 (1999) |
134 | Mesnil, M., Piccoli, C., Tiraby, G., Willecke, K. and Yamasaki, H., Bystander killing of cancer cells by herpes simplex virus thymidine kinase gene is mediated by connexins. Prac. Natl. Acad. Sci. USA, 93,1831-1835 (1996) DOI ScienceOn |
135 | Blakey, D. C., Valcaccia, B. E., East, S., Wright, A. F., Boyle, F. T., Springer, C. J., Burke, P. J., Melton, R.G. and Bagshawe, K.D., Antitumor effects of an antibody-carboxypeptidase G2 conjugate in combination with a benzoic acid mustard prodrug. Cell. Biophys., 22,1-8 (1993) DOI PUBMED |
136 | Rogers, G. T., Burke, P. J., Sharra, S. K., Koode, R. and Boden, J. A., Plasma clearance of an antibody-enzyme conjugate in ADEPT by monoclonal anti-enzyme: its effect on prodrug activation in vivo. Br. J. Cancer, 72, 1357-1363 (1995) DOI PUBMED ScienceOn |
137 | Springer, C. J., Dowell, R., Burke, P. J., Hadley, E., Davies, D. H., Blakey, D. C., Melton, R. G. and Niculescu-Duvaz, I., Optimization of alkylating agent prodrugs derived from phenol nad aniline mustards: a new clincal candidate prodrug (ZD2767) for antibody-directed enzyme prodrug therapy (ADEPT). J. Med. Chem., 38, 5051-5065 (1995) DOI PUBMED |
138 | Tokunaga, Y., Iwasa, T, Fujisaki, J., Sawai, S., Kagayama, A., Liposomal Sustained-Release Delivery Systems for Intravenous Injection. IV. Antitumor Activity of Newly Synthesized Lipophilic 1-b-D-Arabinofuranosylcytosine Prodrug-Bearing Liposomes. Chem. Pharm. Bull., 36, 3574-3583 (1988a) DOI PUBMED ScienceOn |
139 | Uchida, K., Krieis, W., Distribution of 1-b-D-Arabinofuranosylcytosine, Cytidine and Deoxycytidine in Mice Bearing ara-C Sensitive and Resistant P815 Neoplasms. BioChem. Pharmacol., 18, 1115 (1969) DOI ScienceOn |
140 | Wei, S. J., Chao, Y., Shih, Y. L., Yarg, D. M., Hung, Y. M. and Yang, W.K., Involvement of Fas (CD95/APO-1), and Fas ligand in apoptosis induced by ganciclovir treatment of tumor cells transduced with herpes simp ex virus thymidine kinase. Gene Ther., 6, 420-431 (1999) DOI ScienceOn |
141 | Huber, B. E., Austin, E. S., Good, S. S., Knick, V. C., Tibbels, S. and Richards, C. A., In vivo antitumor activity of 5-fluorocytosine on human colorectal carcinoma cells genetically modified to express cytosine deaminase. Cancer Res., 53, 4619-4626 (1993) PUBMED |
142 | McLean, H. M., Heiman, A. S. and Lee, H. J., Synthesis and pharmacological evaluations of novel conjugates of steroidal antedrugs and non-steroidal anti-inflammatory drugs. Med. Chem. Res., submitted (2001) |
143 | Balzarini, J., Holy, A., Jindrich, J., Naesens, L., Snoeck, R., Schols, D., De Clercq E., Differential Antiherpesvirus and Antiretrovirus Effects of the (S) and Enantiomers of Acyclic Nucleoside Phosphonates: Potent and Selective In Vitro and In Vivo Antiretrovirus Activities of (R)-9-(2-Phosphonylme-thoxypropyl)- 2,6-Diaminopurine. Antimicrob. Agents and Chemother., 37, 332-338 (1993) DOI ScienceOn |
144 | Pannecoucke, X., Parmentier, G., Schmitt, G., Dolle, F., Luu, B., Synthesis of the Phosphodiester of 3b(7b-Hydroxycholestrol) and of 5(3Deoxy, 3Azido-thymidine). Tetrahedron, 50, 1173-1178 (1994) DOI ScienceOn |
145 | Topf, N., Worgall, N. R, Hackett, N. R and Crystal, R G., Regional prodrug gene therapy: intravenous administration of an adenoviral vector expressing the E. coli cytosine deaminase gene and systemic administration of 5-fluorocytosine suppresses growth of hepatic metastasis of colon carcinoma. Gene Ther., 5, 507-513 (1998) DOI ScienceOn |
146 | Higuchi, T., Stella, V., Eds. ACS Symp. Ser., no. 14 (1975). Holland, J. F., Glidewell, O., Complementary Chemotherapy in Acute Leukemia. Recent Results Cancer Res., 30, 95 (1970) |
147 | Lefebvre, I., Perigaud, C., Pompon, A., Aubertin, A.M.. Girardet, J.L., Kim, A., Gosselin, G., Imbach, J.L., Mononucleoside Phosphotriester Deravitives with S-Acyl-2-thioethyl Bioreversible Phosphate-Protecting Groups: Intracellular Delivery of 3-Azido-2,3-dideoxythymidine 5-Monophosphate. J. Med. Chem., 38, 3941-3950 (1995) DOI ScienceOn |
148 | Mullen, C. A., Coale, M. M., Lowe, R. and Blaese, R. M., Tumor expressing the cytosine deaminase suicide gene can be eliminated in vivo with 5-fluorocytosine and induce protective immunity to wild type tumor. Cancer Res., 54, 1503-1506 (1994) PUBMED |
149 | Bagshawe, K. D., Sharma, S. K., Springer, C. J. and Rogers, G. T., Antibody-Directed Enzyme Prodrug Therapy (ADEPT): a review of some theoretical, experimental and clinical aspects. Analytical Oncology, 5, 879 (1994) DOI |
150 | Balzarini, J., Aquaro, S., Perno, C.-F., Witvrouw, M., Holy, A, De Clerq, E., Activity of the (R)-Enantiomers of 9-(2Phosphonylmethoxypropyl) adenine and 9-(2-PhosphonyImethoxypropyl)-2,6-Diaminopurine Against Human Immunodeficiency Virus in Different Human Cell Systems. Biochem. Biophys. Res. Comm., 219, 337-341 (1996) DOI ScienceOn |
151 | Periqaud, C., Aubertin, A.M., Benzaria, S., Pelicano, H., Girardet, J.L., Maury, G., Gosselin, G., Kirn, A, Imbach, J.L., Equal Inhibition of the Replication of Human Immunodeficiency Virus in Human T-Cell Culture by ddA Bis (SATE) Phosphotriester and 3-Azido-2,3-dideoxythymidine. Biochem. Pharmacol., 48,11-14 (1994) DOI PUBMED ScienceOn |
152 | Pompon, A., Lefebvre, I., Imbach, J.-L., Khan, S., Farquhar, D.; Antiviral Chem. Chemother., 5, 91-98 (1994) DOI |
153 | Timofeevski, S. L., Panarin, E. F., Vinogradov, O. L. and Nezhentsev, M. V., Anti-inflammatory and antishock watersoluble polyesters of glucocorticoids with low level systemic toxicity. Pharm. Res., 13(3),476-480 (1996) DOI ScienceOn |
154 | Albert, A., Chemical aspects of selective toxicity. Nature, 182, 421-423(1958) DOI PUBMED ScienceOn |
155 | Boyd, M. R., Bacon, T. H., Sutton, D., Antiherpesvirus Activity of 9-(4-Hydroxy-3-hydroxymethylbut-1-yl)guanine (BRL 39123) in Animals. Antimicrob. Agents Chemother., 32, 358-363 (1988) DOI ScienceOn |
156 | Kerr, D. E., Schreiber, G. J., Vrudhula, V. M., Svensson, H. P., Hellstrom, I., Hellstrom, K. E. and Senter, P. D., Regressions and cures of melanoma xenografts following treatment with monoclonal antibody beta-lactamase conjugates in combination with anticancer prodrugs. Cancer Res., 55, 3558-3563 (1995) PUBMED |
157 | Meier, C. 4H-1.3.2.-Benzodioxaphosphorin-2-nucleosyl-2-oxide A New Concept for Lipophilic, Potential Prod rugs of Biologically Active Nucleoside Monophosphates. Angew. Chem., 108, 77-79 (1996) DOI |
158 | Meier, C., Lorey, M., De Clerq, E., Balzarini, J., Cyclic Saligenyl Phosphotriesters of 2,3-Dideoxy-2,3-didehydrothymidine (d4T)-A New Pro-nucleotide Approach. Bioorg. Med. Chem. Lett., 7, 99-104 (1997b) DOI ScienceOn |
159 | Melton, R. G., Searle, F.,Sherwood, R. F., Bagshawe, K. D. and Boden, J. A., The potential of carboxypeptidase G2 antibody conjugates as anti-tumour agents. II. In vivo localizing and clearance properties in a choriocarcinoma model. Br. J. Cancer, 61, 420-424 (1990) DOI PUBMED ScienceOn |
160 | Moolten, F. L., Tumor chemotherapy conferred by inserted herpes thymidine kinase genes: paradigm for a prospective cancer control strategy. Cancer Res., 46,5276-5281 (1986) PUBMED |
161 | Perigaud, C., Gosselin, G., Benzaria, S., Girardet, J.L., Maury, G., Pelicano, H., Aubertin, A.M., Kirn, A., Imbach, J.L., Bis(S-Acyl-2Thioethyl)esters of 2,3-Dideoxyadenosine 5Monophosphate are Potent Anti-HIV Agents il Cell Culture. Nucleosides & Nucleotides, 14,789-791 (1995) DOI ScienceOn |
162 | Shand, N., Weber, F., Mariani, L., Bernstein, M., Gianella-Borradori, A., Long, Z., Sorensen, A G. and Barbier, N., A phase 1-2 clinical trial of gene therapy for recurrent glioblastoma multiforme by tumor: transduction with herpes simplex thymidine kinase gene followed by ganciclovir. Hum. Gene Ther., 10, 2325-2335 (1999) DOI ScienceOn |
163 | Fiorino, T., Current and future treatment of inflammatory bowel disease. Drug & Market Development. 42-48 (2000) |
164 | Khalil, M. A., Maponya, M. F., Ko, D.-H., You, Z., Oriaku, E. T. and Lee, H. J., New antiinflammatory steroids: [16a,17a-d]-3hydroxyiminoformylisoxazoline derivatives of prednisolone and 9a-fluoroprednisolone. Med. Chem. Res., 6, 52-60 (1996) |
165 | Barnes, P. J., Anti-inflammatory actions of glucocorticoids: molecular mechanisms. Clinical Science, 94, 557-572 (1998) DOI |
166 | Beltinger, C., Fulda, S., Kammertoens, T., Uckert, Wand Debatin, K. M., Mitochondrial amplification of death signals determines thymidine kinase/ganciclovir-triggered activation of apoptosis. Cancer Res., 60, 3213-3217 (2000) |
167 | Frishman, W. H. and Hershman, D., Beta-adrenergic blocking drugs in cardiac disorders. In Cardiovascular Drug Therapy, 2nd ed., Messerli, F. H., Ed.; W B. Saunders Co., New York, 465-474 (1996) |
168 | McGuigan, C., Pathirana, R. N., Balzarini, J., De Clercq, E, Intracellular Delivery of Bioactive AZT Nucleotides by Aryl Phosphate Derivatives of AZT J. Med. Chem., 36, 1048-1052 (1993) DOI ScienceOn |
169 | McGuigan, C., Tsang, H.-W., Cahard, D., Turner, K., Velazquez, S., Salgado, A., Bidois, L., Naesens, L., De Clercq, E., Balzarini, J., Phosphoramidates Derivatives of d4T as Inhibitors of HIV: The Effect of Amino Acid Variation. Antiviral Res., 35,195-204 (1997b) DOI ScienceOn |
170 | Sakai, A., Mori, N., Shuto, S., Suzuki, T., Deacylation-Reacylation Cycle: A Possible Absorption Mechanism for the Novel Lymphotropic Antitumor Agent Dipalmitoylphosphatidylfluorouridine in Rats. J. Pharm. Sci., 83, 575-578 (1993) |
171 | Shuto, S., Itoh, H.; Ueda, S., Imamura, S., Fukukawa, K., Tsujino, M., Matsuda, A, Ueda, T, A Facile Enzymatic Synthesis of 5-(3-sn-Phosphatidyl)nucleosides and Their Antileukemic Activities. Chem. Pharm. Bull., 36, 209-217 (1988) DOI PUBMED ScienceOn |
172 | Svensson, H. P., Frank, I. S., Berry, K. K. and Senter, P.D., Therapeutic effects of monoclonal antibody-b-lactamase conjugates in combination with a nitrogen mustard anticacer prodrug in models of human renal cell carcinoma. J. Med. Chem., 41,1507-1512 (1998) DOI ScienceOn |
173 | Svensson, H. P., Kadow, J. F., Vrudhula, V. M., Wallace, P. M. and Senter, P. D., Monoclonal antibody-b-lactamase conjugates for the activation of a cephalosporin mustard prodrug. Bioconjug. Chem., 3,176-181 (1992) DOI PUBMED |
174 | Mar, E., C., Chiou, J. F., Cheng, Y. C. and Huang, E. S., Human cytomegalovirus-indeced DNA polymerase and its interaction with the triphosphates of 1-(2-deoxy-2-fluoro-beta-Darabinofuranosyl)- 5-methyuracil, -5-iodocytosine, and 5methylcytosine. J. Virol., 56, 846-851 (1995) |
175 | Austin, E. A. and Huber B. E., A first step in the development of gene therapy for colorectal carcinoma: cloning, sequencing, and expression of E. coli cytosine deaminase. Mol. Pharmacol. 43, 380-387 (1993) PUBMED |
176 | Bagshawe, K. D., Springer, C. J. Searle, F., Antoniw, P., Shama, S. K., Melton, R. G. and Sherwood, R. F., A cytotoxic agent can be generated selectively at cancer sites. Br. J. Cancer, 58, 700-703 (1988) DOI PUBMED ScienceOn |
177 | Tanaka, T., Kanai, F., Okabe, S., Yoshida, Y., Wakimoto, H., Hamada, H., Shiratori, Y., Lan, K.-H., Ishitobi, M. and Ornata, M., Adenovirus-mediated prodrug gene therapy for carcinoembryonic antigen-producing human gastric carcinoma cells in vitro. Cancer Res., 56, 1341-1345 (1996) PUBMED |
178 | Giradet, J.L., Gosselin, G., Perigaud, C., Balzarini, J., De Clercq, E., Imbach, J.-L., Nucleosides & Nucleotides, 14, 645-647 (1995a) DOI ScienceOn |
179 | Harden, M. R., Jarvest, R. L., Boyd, M. R., Sutton, D., Vere Hodge, R. A., Prodrugs of Selective Antiherpesvirus Agent 9-[4-Hydroxy-3-(hydroxymethyl)but-1-yl]guanine (BRL 39123) with Improved Gastrointestinal Absorption Properties. J. Med. Chem., 32,1738-1743 (1989) DOI PUBMED |
180 | Heiman, A. S., Hickman, F., Ko, D.-H. and Lee, H. J., New steroidal anti-inflammatory antedrugs bind to macrophage glucocorticoid receptors and inhibit nitric oxide generation. Steroids, 63, 644-649 (1998) DOI ScienceOn |
181 | Bodey, G. P., Freireich, E. J., Monto, R. W, Hewlett, J. S., Cytosine Arabinoside (NSC-63878) Therapy For Acute Leukemia in Adults. Cancer Chemother. Rep., 53, 59 (1969) PUBMED |
182 | You, Z., Heiman, A S., Chen, M. and Lee, H. J., Novel steroid spiro enones: Consideration of prednisolone derivatives with diethyl oxalate. Steroids, 65, 109-115 (2000) DOI ScienceOn |
183 | Eltahir, A., Heys, S. D., Hutcheon, A. W., Sarkar, T. K., Smith, I., Walker, L. G., Ah-See, A. K. and Eremin, O., Treatment of large and locally advanced breast cancers using neoadjuvant chemotherapy. Am. J. Surg., 175, 127-132 (1998) DOI ScienceOn |
184 | Fridland, A., Robbins, B. L., Srinivas, R. V.. Arimilli, M., Kim, C., Bischofberger, N., Antiretroviral Activity and Metabolism of bis(POC)PMPA, an Oral Bioavailable Prodrug of PMPA. Antiviral Res., 34, A49, 27 (1997) DOI ScienceOn |
185 | Myles, M. H., Bischofberger, N., Hoover, E A., Evaluation of 9( 2-Phosphonyl-methoxypropyl)adenine Antiviral Therapy for Acute Feline Immunodeficiency Virus Infection in Cats. 3rd International Feline Retrovirus Research Symposium 1996, Fort Collins, Col. USA |
186 | Perigaud, C., Gosselin, G., Imbach, J.L., Minireview: from the Pronucleotide Concept to the SATE Phosphate Protecting Groups. Curr. Topics in Med. Chem., 2, 15-29 (1997) |
187 | Balzarini, J., Egberink, H., Hartmann, K., Cahard, D., Vahlenkamp, T., Thormar, H., De Clercq, E, McGuigan, C., Antiretrovirus Specificity and Intracellular Metabolism of 2,3-Didehydro-2,3-dideoxythymidine (Stavudine) and Its 5-Monophosphate Triester Prodrug S0324. Mol. Pharmacol., 50, 1207-1213 (1996b) PUBMED |
188 | Biggadike, K., Lynn, S. M., Procopiou, P. A., Shaw, R. E. and Williamson, C. J. Chem. Soc., Perkin Trans. 1, 813-818 (2000) |
189 | Hwang, S. K., Juhasz, A., Yoon, S. H. and Bodor, N., Design, synthesis and evaluation of soft bufuralol analogues. J. Med. Chem., 43(8), 1525-1532 (2000) DOI ScienceOn |
190 | Dessolin, J., Vlieghe, P, Bouygues, M., Medou, M., Quelever, G., Camplo, M., Chermann, J. C., Kraus, J. L., Tri-N-Boc-Tetraazamacrocycle- Nucleoside Conjugates: Synthesis and Anti-HIV Activities. Nucleosides & Nucleotides, 17, 957-968 (1998) DOI PUBMED ScienceOn |
191 | Ji Y., Moog, C., Schmitt, G., Bischoff, P., Luu, B., Monophosphoric Acid Diesters of 7b Hydroxycholestrol and of Pyrimidine Nucleosides as Potential Antitumor Agents: Synthesis and Preliminary Evaluation of Antitumor Activity. J. Med. Chem., 33, 2264-2270 (1990) DOI PUBMED |
192 | Kaneko, Y. and Tsukamoto, A., Gene therapy of hepatoma: bystander effects and non-apoptotic cell death induced by thymidine kinase and ganciclovir. Cancer Lett., 96, 105-110 (1995) DOI ScienceOn |
193 | Meier, C., Lorey, M., De Clerq, E, Balzarini, J., CycloSal-2,3-dideoxy-2,3-didehydrothymidine Monophosphate (CycloSal-d4TMP): Synthesis and Antiviral Evaluation of a New d4TMP Delivery System. J. Med. Chem., 41, 1417-1427 (1998) DOI ScienceOn |
194 | Balzarini, J., Kruining, J., Wedgwood, O., Pannecouque, C., Aquaro, S., Perno, C.F., Naessens, L., Witvrouw, M., Heijtink, R., De Clercq, E., McGuigan, C., Conversion of 2, 3Dideoxyadenosine (ddA) and 2, 3-Didehydro-2, 3-dideoxyadenosine (d4A) to Their Corresponding Aryloxyphosphoramidate Derivatives Markedly Potentiates Their Activity Against Human Immunodeficiency Virus and Hepatitis B Virus. FEBS Letters, 410, 324-328 (1997) DOI PUBMED ScienceOn |