• Title/Summary/Keyword: Platinum(II) complex

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Dichloro Platinum (II) Complex of S-6,6'-Dimethyl-2,2'-diaminobiphenyl (S-6,6'-Dimethyl-2,2'-diaminobiphenyl 리간드의 디클로로백금 (II) 착물)

  • Moo-Jin Jun;Sung-Rack Choi
    • Journal of the Korean Chemical Society
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    • v.28 no.6
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    • pp.399-402
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    • 1984

  • The S-enantiomer of the 6,6'-dimethyl-2,2'-dia minobiphenyl (dmdabp) has been obtained by resolving dmdabp with l-tartaric acid. The square planar dichloro platinum(II) complex has been prepared with the optically active S-dmdabp, which is found to take the conformation in the [Pt(S-dmdabp)Cl$_2]$ complex.

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제3세대 백금착체 항암제 신약개발 1. Design, synthesis and antitumor activity of 3rd generation platinum complexes.

  • 김대기;김강혁;김종식;주상섭;김기협;김노경
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1993.04a
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    • pp.73-73
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    • 1993

  • As part of a research program to develope 3rd generation anti tumor platinum complexes, a series of platinum complexes which have 4, 5-bis-(aminomethyl)- 1, 3-dioxolane derivatives as bidenate amine ligands, represented by the general structual formula was prepared. The R$_1$ and/or R$_2$ substituents in this series of platinum complexes can be hydrogen. alkyl, of jointly formed cyclohexane. Two Xs can be a bidenate leaving ligand such as 1, 1-cyclobutanedicarboxylate, malonate, dimethylmalonate, ethylmalonate, glycolate, L-lactate, or N-methyliminodiacetate. From based on the pharmacological and toxicological studies, we have chosen SKI 2053R, cis-malonato[(4R, 5R)-4, 5-bis(aminomethyl)-2-isopropyl-1, 3-dioxolane] platinum(II) complex (NSC D644591) as a candidate for clinical evaluation. The antitumor activity of a new anti tumor platinum complex, cis-malonato [(4R, 5R)-4, 5-bis(aminomethyl)-2-isopropyl-1, 3-dioxolane] platinum(II) (SKI 2053R, NSC D644591), was compared with those of cisplatin and carboplatin using murine tumors. We evaluated three platinum complexes against L1210/CPR, a subline of L1210 leukemia resistant to cisplatin for their abilities to overcome tumor resistance to cisplatin. The in vitro cytotoxicity of SKI 2053R to L1210 cell line was 2.5-fold less potent thann that of cisplatin, and was 10-fold more cytotoxic than that of carboplatin. SKI 2053R retained similar cytotoxic effect and anti tumor activity to L1210/CPR cell line, like the cytotoxicity of SKI 2053R to L1210 cell line, while either cisplatin or carboplatin had not property to overcome the acquired cisplatin-resistance. SKI 2053R exhibited greater or comparable antitumor activity than cisplatin or carboplatin in murine tumor models.

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In vitro Antitumor Activity and Nephrotoxicity of Pt(II) Complexes Containing Diaminocyclohexane

  • Hong, Eon-Pyo;Rho, Young-Soo;Jung, Jee-Chang
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.358.2-358.2
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    • 2002

  • Platinum(II) coordination complex(cisplatin) has been currently used as one of the most effective compounds in the treatment of various solid tumors. However. its use has been limited by severe side effects such as renal toxicity. Our platinum-based drug discovery program has been aimed at developing drugs capable of diminishing toxicity and improving selective cytotoxicity. (omitted)

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Studies on the Hemolytic Mechanism of Antitumor Platinum Complex (항암성 백금화합물의 용혈독성기전에 관한 연구)

  • 최병기;박영숙;정세영
    • Environmental Analysis Health and Toxicology
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    • v.8 no.3_4
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    • pp.33-41
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    • 1993

  • This study was designed to determine the hemolytic mechanism of antitumor agent tetraphosphine platinum (II) complex (RC-1), which was synthesized recently. Erythrocytes treated with RC-1 showed concentration and time dependent lipid peroxydation, methemoglobin synthesis and hemolysis. And also treatment of radical scavengers showed the inhibitory effect of hemolysis and the decrease of malondialdehyde levels in RC-1 treated erythrocytes. So, the mechanism of hemolysis was considered to be the generation of free radicals, methemoglobin synthesis and the lipid peroxidation of phospholipid which composed of erythrocyte membrane.

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Determination of Stability Constants Using Electrochemical Methods for the Complex Formation of Platinum and Palladium with Polyelectrolytes

  • Park, Joon Seo;Chung, Koo Soon
    • Analytical Science and Technology
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    • v.8 no.4
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    • pp.691-698
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    • 1995

  • The complexation of platinum and palladium with synthetic polyelectrolytes was studied. The successive and overall stability constants of Pd(II) with PEI and 2PVP were obtained by potentiometric titration. Because of the slow equilibrium time, the potentiometric titrations were performed using the home-made automatic titrator in order to analyze the complexations according to the modified Bjerrum method. The complex formation constant of Pt(IV) with 2PVP, measured by differential pulse polarography, was calculated from the peak currents that were obtained in non-complexing media and in solution containing 2PVP.

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