• 제목/요약/키워드: Biological Synthesis

검색결과 1,240건 처리시간 0.038초

Novel $\delta$-Lactam base Histone Deacetylase Inhibitors: Synthesis and Biological Evaluation I.

  • Park, Bum-Woo;Ryu, Dong-Kyu;Kim, Tae-Kyun;Park, Song-Kyu;Han, Jeong-Hwan;Han, Gyoon-Hee
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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    • pp.184.1-184.1
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    • 2003
  • HDAC and HAT (histone acetyltransferase) are involved in co-regulation in chromatin remodeling and the functional regulation of gene transcription. Abnormal recruitment of HDAC is related to carcinogenesis. Thus, the identification of potent histone deacetylase (HDAC) inhibitor has been considered as very intriguing approach for development for cancer chemotherapy. More recently, anti-inflammatory activity of SAHA cytokines was reported via reduction of proinflammatory cytokinres in vitro and in vivo. (omitted)

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Stereoselective synthesis of novel 4′$\alpha$-C-methyl branched novel carbocyclic nucleosides

  • Kim, Ji-Hee;Ko, Ok-Hyun;Hong, Joon-Hee
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.345.2-345.2
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    • 2002
  • Recently. 4'${\alpha}$-C homologated furanose nucleosides. especially alkyl branches. are molecules of considerable current interest. One of reasons for this prominence arises from the notable biological activities as antiviral and antitumor agents. as shown in 4'${\alpha}$-C-methyl-2-deoxythymidine (EC$_{50}$ = 7.2$\mu$M against HIV in MT-4 cell), 4'${\alpha}$-C-fluoromethyl-2-deoxycytidine. 4'${\alpha}$-C-hydroxymethylthymidine and 4'${\alpha}$- -C-azidomethyl-thymidine. (omitted)omitted)

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DESIGN, SYNTHESIS AND IN VITRO EVALUATION OF APIO ANALOGUE OF NEPLANOCIN A

  • Moon, Hyung-Ryong;Lee, Jeong-Ah;Yoo, Byul-Nae;Shin, Dae-Hong;Jeong, Lak-Shin
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.233.2-233.2
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    • 2002
  • Apio nucleosides whose 4'-hydroxymethyl group moves to 3'-position exhibit interesting biological activity such as antitumor or antiviral activity. On the other hand. neplanocin A is the representative of the carbocyclic nucleosides and has been recognized as a potent antitumor and antiviral agent. Based on these findings. it was of great interest to design apio neplanocia A which combined the properties of apio nucleosides and neplanocin A. (omitted)

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Synthesis of 2,6-Diaromatic Substituted Pyridine Derivatives and Their Antitumor Activities

  • Moon, Yoon-Soo;Lim, Hyun-Tae;Zhao, Long-Xuan;Basnet-Arjun;Lee, Eung-Seok
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.345.1-345.1
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    • 2002
  • ${\alpha}$-terthienyl the first isolated from natural products shows potent antitumor activity, which encouraged us to study terpyridine and its biological properties. Terpyridine has also been reported as having carcinogenicity, and it's erivatives showed high cytotoxic activities against several human cancer cell lines and topoisomerase I inhibitory ctivity. Mannich free base from condensation reaction was allowed to react with pyridinum salts to give activity. (omitted)

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Straightforward synthesis of 4'${\alpha}$-C-hydroxymethyl branched novel carbocyclic nucleosides

  • Oh, Jung-Hyo;Kim, Kwan-Woo;Hong, Joon-Hee
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.354.1-354.1
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    • 2002
  • Carbocyclic nucleosides are unique class in which a methylene group replaces the oxygen in the furan, which result in metabolic stability to endogenous phosphorylase. The biologically active natural carbocyclic nucleosides such as aristeromycin and neplanocin were found to possess interesting biological properties including antiviral and antitumor activity. (omitted)

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Total synthesis of Antofine by using Intramolecular 1.3-dipolar cycloaddition of Azidealkene

  • Lee, Jae-Kwang;Lee, Tae-Ho;Song , So-Young
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.362.2-362.2
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    • 2002
  • Antofine belongs to the Phenathroindolizidine group of alkaloids. This natural products exhibit interesting biological properties such as antitumour activity. and anti-inflammentory. Wittig reaction of phenathrenealdehyde with the phosponium salt provided the phenathreneazidealkene in good yield. Intramolecular 1.3-dipolar cycloaddition of the resulting azidealkent in refluxing benzene proceeded the imine. It was reduced with cyanoborohydride of Noyori's Asymmetric Hydrogenation. (omitted)

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Synthesis and Biological Evaluation of Pyrimidine Nucleosides Fused with 3′,4′- Tetrahydrofuran Ring

  • Kim, Myong-Jung;Chung, Soon-Yong;Liang, Cheng-Wu;Chun, Moon-Woo
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.363.2-363.2
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    • 2002
  • A number of 2',3'-deoxynucleosides have been discovered to possess significant antiviral activity against HIV-1 and other viruses. Since it has been suggested that proper conformation of the dideoxynucleosides in terms of ring puckering of the five-membered sugar moiety is required for them to exhibit antiviral activity a number of nucleoside analogues to fix sugar-ring puckering have been synthesize and evaluated for antiviral activity. (omitted)

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Synthesis and Biological Activities of New Substituted Indoles

  • Hishmat, Orchidee H.;Nakkady, Sally S.;El Shabrawy, Osama A.;Mahmoud, Sawsan S.
    • Archives of Pharmacal Research
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    • 제15권1호
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    • pp.104-108
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    • 1992
  • 2, 3-Diphenyl-6-formyl-5-methoxyindole reacts with ethyl cyano acetate to yield the arylidene derivative which forms with urea and thiourea the corresponding pyrimidine derivatives. The arylidene derivatives react with hydrazines and with active methylenes to form the respective pyrazole derivatives and the $\alpha, \;\beta$-disubstituted acrylonitriles. Seven new compounds were tested for their effects on the arterial blood pressure of rats and analgesic activity.

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Comparative Toxicity Studies of Ultra-Pure Ag, Au, Co, and Cu Nanoparticles Generated by Laser Ablation in Biocompatible Aqueous Solution

  • Kim, Yea-Seul;Kim, Kuk-Ki;Shin, Seon-Mi;Park, Seung-Min;Hah, Sang-Soo
    • Bulletin of the Korean Chemical Society
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    • 제33권10호
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    • pp.3265-3268
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    • 2012
  • Nanoparticles (NPs) are increasingly used in consumer products, which have aroused many concerns and debates regarding their fate in biological systems from a point of their safety/toxicity. Although a number of studies on the biological effects of NPs have been published, these are often complicated by the possible toxicity of conventional NPs, caused by contamination with chemical precursors or additives during their synthesis and/or purification procedures. To explicitly understand the toxicity basis of NPs, it is necessary to directly address a main problem related to their intrinsic/inherent toxicity and/or incompatibility with biological objects. The present study is designed to take advantage of a novel laser-assisted method called laser ablation to generate Ag, Au, Co, and Cu NPs in biocompatible aqueous solution, and to evaluate the toxicity of the resulting ultra-pure NPs. Our results show that the ultra-pure NPs with nascent surfaces possess moderate cytotoxicity to human cells in a cell-dependent manner.

Design, Synthesis and Biological Evaluation of Novel Analogs of Bortezomib

  • Rao, R. Janaki Rama;Rao, A.K.S. Bhujanga;Swapna, K.;Rani, B. Baby;Kumar, S. Prasanna;Awantika, S.;Murthy, Y.L.N.
    • 대한화학회지
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    • 제55권5호
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    • pp.765-775
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    • 2011
  • Novel analogs of bortezomib were designed, synthesized and in vitro biological evaluation was carried out using human tumor cell lines A549 and PC3. Docking studies of these analogs of bortezomib was discussed. According to biological investigations, the inhibitors 4, 6, and 8 were found to be more potent than reference drug candidate bortezomib. A549 cell line showed significant sensitivity towards 4, 6, and 8 with $IC_{50}$ values 14.03, 18.5, and 12.4 nM, respectively, and PC3 cell line showed IC50 values 26.1, 37.0, and 21.2 nM, respectively. The $IC_{50}$ values of bortezomib in these cell lines are 27.3 nM and 42.0 nM.