Synthesis and anticancer activity of lipophilic platinum(II) complexes of 3,5-diisopropylsalicylate
Yu, Yao1; Lou, Li-Guang2; Liu, Wei-Ping1; Zhu, Hua-Jie3; Ye, Qing-Song1; Chen, Xi-Zhu1; Gao, Wen-Gui1; Hou, Shu-Qian1
2008-07-01
发表期刊EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
ISSN0223-5234
卷号43期号:7页码:1438-1443
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.
关键词Lipophilic Platinum(Ii) Complexes Antitumor Activity 3 5-diisopropylsalicylic Acid
学科领域Chemistry, Medicinal
DOI10.1016/j.ejmech.2007.09.006
收录类别SCI
语种英语
WOS研究方向Pharmacology & Pharmacy
WOS类目Chemistry, Medicinal
WOS记录号WOS:000258250700010
引用统计
被引频次:26[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/2923
专题植物化学与西部植物资源持续利用国家重点实验室
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
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Yu, Yao,Lou, Li-Guang,Liu, Wei-Ping,et al. Synthesis and anticancer activity of lipophilic platinum(II) complexes of 3,5-diisopropylsalicylate[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2008,43(7):1438-1443.
APA Yu, Yao.,Lou, Li-Guang.,Liu, Wei-Ping.,Zhu, Hua-Jie.,Ye, Qing-Song.,...&Hou, Shu-Qian.(2008).Synthesis and anticancer activity of lipophilic platinum(II) complexes of 3,5-diisopropylsalicylate.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,43(7),1438-1443.
MLA Yu, Yao,et al."Synthesis and anticancer activity of lipophilic platinum(II) complexes of 3,5-diisopropylsalicylate".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 43.7(2008):1438-1443.
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