文章基本信息

标题：Selective Cytotoxicity Platinum ( II )Complex Contaning Carrier Ligand of cis - 1,2 - Diaminocyclohexane
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作者：Young - Soo Rho ; Se - Young Choung ; Jee- Chang Jung 等
期刊名称：Environmental Health and Toxicology
电子版ISSN：2233-6567
出版年度：1998
卷号：13
期号：2
语种：English
出版社：Korean Society of Environmental Health and Toxicology
摘要：The use of cisplatin is limited by severe side effects such as renal toxicity. Our platinum-base drug discovery is aimed at developing drugs capable of diminishing toxicity and improving antitumor activity. We synthesized new Pt (II) complex analogue [Pt (cis- DACH)(DPPP)] . 2NO (PC) containing cis-1,2 -diaminocyclohexane as a carrier ligand and 1,3- bis( diphenylphosphino) propane as a leaving group. Furthermore,nitrate was added to improved the solubility. In this study. its structure was determined and its antitumor activity against SKOV -3 and NIH-OVCAR -3 human ovarian adenocarcinoma,and in vitro cytotoxicity was determined against primary cultured rabbit kidney proximal tubular and renal cortical cells of human kidney using colorimetric MTT assay. PC demonstrated acceptable antitumor activity against SKOV-3 and NIH -OVCAR -3 human ovarian adeno- carcinoma and significant activity as compared with that of cisplatin. The toxicity of PC was found quite less than that of cisplatin using MTT and H- thymidine uptake tests in rabbit proximal tubular cells and human kidney cortical cells. PC was used for human cortical tissue in 7 weeks hitoculture by the glucose -consumption tests. We determined that the new platinum drug has lower nephrotoxicity than cisplatin. Based on these results. this novel platinum (II) complex compound (PC) represent a valuable lead in the development of a new anticancer chemotherapeutic agent capable of improving antitumor activity and low nephrotoxicity 。.