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Synthesis, anticancer activity and toxicity of a water-soluble 4S,5S-derivative of heptaplatin, cis-{Pt(II)[(4S,5S)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane].(3-hydroxyl-cyclobutane-1,1-dicarboxylate)}

文献类型：期刊论文

作者Liu, Weiping1; Jiang, Jing1; Xie, Chengying2; Hou, Shuqian1; Quan, Haitian2; Ye, Qingsong1; Lou, Liguang2
刊名JOURNAL OF INORGANIC BIOCHEMISTRY
出版日期2014-11
卷号140页码:126-130
ISSN号0162-0134
关键词Platinum complexes Anticancer activity Toxicity Heptaplatin Derivative
DOI10.1016/j.jinorgbio.2014.07.013
文献子类Article
英文摘要A water-soluble 4S,5S-derivative of heptaplatin, cis-{Pt(II)[(4S,5S)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane]center dot(3-hydroxyl-cyclobutane-1,1-dicarboxylate)} was synthesized. The anticancer activity and toxicity were evaluated by comparing its interaction with DNA, cytotoxicity against four human cancer cell lines, antitumor efficiency in human gastric carcinoma NCI-N87 xenografts in nude mice, and preliminary side-effects in rats to those of its 4R,5R-optical isomer which is under preclinical development. Both isomers induce condensation of DNA to the same extent and have similar cytotoxicity, but show different antitumor activity and toxicity, probably owing to the difference in respective pharmacokinetic profiles. 4S,5S-Isomer seems to exhibit superior antitumor activity and less toxicity than 4R,5R-optical isomer as well as the parent heptaplatin. These results imply that 4S,5S-configuration as a new drug candidate may be better than 4R,5R-counterpart. (C) 2014 Elsevier Inc. All rights reserved.
WOS关键词ANTITUMOR-ACTIVITY ; PLATINUM COMPLEXES ; IN-VITRO ; CISPLATIN ; DESIGN ; AGENTS ; DRUGS ; CANCER ; DICHLOROACETATE ; CYTOTOXICITY
资助项目Natural Science Foundation of China[21161010] ; National Key R&D Program of China[2012BAE06B08] ; National Key R&D Program of China[2009ZX09103-109]
WOS研究方向Biochemistry & Molecular Biology ; Chemistry
语种英语
出版者ELSEVIER SCIENCE INC
WOS记录号WOS:000342608900016
源URL[http://119.78.100.183/handle/2S10ELR8/276861]  
专题药理学第一研究室
通讯作者Lou, Liguang
作者单位1.Kunming Inst Precious Met, State Key Lab Platinum Grp Met, Kunming 650106, Yunnan, Peoples R China;
2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Liu, Weiping,Jiang, Jing,Xie, Chengying,et al. Synthesis, anticancer activity and toxicity of a water-soluble 4S,5S-derivative of heptaplatin, cis-{Pt(II)[(4S,5S)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane].(3-hydroxyl-cyclobutane-1,1-dicarboxylate)}[J]. JOURNAL OF INORGANIC BIOCHEMISTRY,2014,140:126-130.
APA Liu, Weiping.,Jiang, Jing.,Xie, Chengying.,Hou, Shuqian.,Quan, Haitian.,...&Lou, Liguang.(2014).Synthesis, anticancer activity and toxicity of a water-soluble 4S,5S-derivative of heptaplatin, cis-{Pt(II)[(4S,5S)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane].(3-hydroxyl-cyclobutane-1,1-dicarboxylate)}.JOURNAL OF INORGANIC BIOCHEMISTRY,140,126-130.
MLA Liu, Weiping,et al."Synthesis, anticancer activity and toxicity of a water-soluble 4S,5S-derivative of heptaplatin, cis-{Pt(II)[(4S,5S)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane].(3-hydroxyl-cyclobutane-1,1-dicarboxylate)}".JOURNAL OF INORGANIC BIOCHEMISTRY 140(2014):126-130.

入库方式： OAI收割

来源：上海药物研究所

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