Abstract
The dinuclear platinum complex bis(acetato)diammine-bis-μ-acetato diplatinum (II) dihydrate has been previously shown to exert profound cytotoxicity in diverse tumor cell lines, while being far less detrimental than the clinically applied platinum drugs against some susceptible to platinum toxicity non-malignant cellular populations. In the present study we report the investigation of the cellular accumulation kinetics and apoptosis induction of the dinuclear complex in K-562, its potent in vivo antineoplastic activity against L1210 leukemia and Lewis lung carcinoma tumor models and its lower nephrotoxicity, myelosuppresive potential and clastogenicity in vivo relative to cisplatin.
Keywords: Dinuclear platinum complexes, K-562, L-1210 leukemia, Lewis lung carcinoma, nephrotoxicity, genotoxicity
Medicinal Chemistry
Title: Cellular Pharmacology, Antineoplastic Activity and Low In Vivo Toxicity of a Carboxylato-Bridged Platinum(II) Complex bis(acetato)diammine-bis-μ-acetato diplatinum (II) Dihydrate
Volume: 3 Issue: 2
Author(s): Georgi Momekov, Spiro Konstantinov, Margarita Topashka-Ancheva, Adriana Bakalova, Sonja Arpadjan and Margarita Karaivanova
Affiliation:
Keywords: Dinuclear platinum complexes, K-562, L-1210 leukemia, Lewis lung carcinoma, nephrotoxicity, genotoxicity
Abstract: The dinuclear platinum complex bis(acetato)diammine-bis-μ-acetato diplatinum (II) dihydrate has been previously shown to exert profound cytotoxicity in diverse tumor cell lines, while being far less detrimental than the clinically applied platinum drugs against some susceptible to platinum toxicity non-malignant cellular populations. In the present study we report the investigation of the cellular accumulation kinetics and apoptosis induction of the dinuclear complex in K-562, its potent in vivo antineoplastic activity against L1210 leukemia and Lewis lung carcinoma tumor models and its lower nephrotoxicity, myelosuppresive potential and clastogenicity in vivo relative to cisplatin.
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Momekov Georgi, Konstantinov Spiro, Topashka-Ancheva Margarita, Bakalova Adriana, Arpadjan Sonja and Karaivanova Margarita, Cellular Pharmacology, Antineoplastic Activity and Low In Vivo Toxicity of a Carboxylato-Bridged Platinum(II) Complex bis(acetato)diammine-bis-μ-acetato diplatinum (II) Dihydrate, Medicinal Chemistry 2007; 3 (2) . https://dx.doi.org/10.2174/157340607780059486
DOI https://dx.doi.org/10.2174/157340607780059486 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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