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题名: Synthesis and anticancer activity of lipophilic platinum(II) complexes of 3,5-diisopropylsalicylate
作者: Yu, Yao1; Lou, Li-Guang2; Liu, Wei-Ping1; Zhu, Hua-Jie3; Ye, Qing-Song1; Chen, Xi-Zhu1; Gao, Wen-Gui1; Hou, Shu-Qian1
刊名: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
关键词: lipophilic ; platinum(II) complexes ; 3,5-diisopropylsalicylic acid ; antitumor activity
英文摘要: Novel lipophilic platinum(II) complexes (LSPt-1-3). containing 3,5-diisopropylsalicylate (DIPS) as a leaving group and 2NH(3) or 1R,2R-diaminocyclohexane or (4R,5R)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane as the carrier, have been synthesized, characterized and evaluated in vitro and in vivo. The octanol/water distribution coefficient of the complexes has also been measured. The results showed that the complexes achieved a typical square planar and the octanol/water distribution coefficient log P was 4.27, 4.37 and 4.31. The complexes were tested by SRB method to be more cytotoxic than Carboplatin, Oxaliplatin and Eptaplatin against 3AO, A549, NCI-H460 and SGC-7901 human cancer cell lines. Among complexes, LSPt-2 was much more effective than Carboplatin and Oxaliplatin in treating the NCI-H460 non-small-cell lung tumor-bearing mice. Its optimal activity was 38.8% (T/C) at a dose of 30 mg/kg following i.p. administration. LD50 for the complex was found to be 230.9 mg/kg. LSPt-2 exhibited great anticancer activity, good lipophilic ability and low toxicity and therefore, it is a promising candidate for effective and stable pharmaceutical liposomal platinum anticancer drug. (c) 2007 Elsevier Masson SAS. All rights reserved.
出版日期: 2008-07-01
卷号: 43, 期号:7, 页码:1438-1443
DOI标识: 10.1016/j.ejmech.2007.09.006
语种: 英语
收录类别: SCI
学科分类: Chemistry, Medicinal
ISSN号: 0223-5234
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内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/2923
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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作者单位: 1.Kunming Inst Precious Met, Platinum Based Drug Lab, Kunming 650221, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
3.Chinese Acad Sci, Kunming Inst Bot, Kunming 650204, Peoples R China

Recommended Citation:
Yu, Y; Lou, LG; Liu, WP; Zhu, HJ; Ye, QS; Chen, XZ; Gao, WG; Hou, SQ.Synthesis and anticancer activity of lipophilic platinum(II) complexes of 3,5-diisopropylsalicylate,EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2008,43(7):1438-1443
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