Design, synthesis and anticancer activity of diam(m)ine platinum(II) complexes bearing a small-molecular cell apoptosis inducer dichloroacetate

doi:10.1016/j.jinorgbio.2015.02.002

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	Design, synthesis and anticancer activity of diam(m)ine platinum(II) complexes bearing a small-molecular cell apoptosis inducer dichloroacetate
	Liu, Weiping 2; Jiang, Jing 2; Xu, Yongping 1; Hou, Shuqian 2; Sun, Liping 1; Ye, Qingsong 2; Lou, Liguang1
刊名	JOURNAL OF INORGANIC BIOCHEMISTRY
	2015-05
卷号	146 页码:14-18
关键词	Platinum complexes Anticancer activity Drug resistance Dichloroacetate
ISSN号	0162-0134
DOI	10.1016/j.jinorgbio.2015.02.002
文献子类	Article
英文摘要	Four new diam(m)ine platinum complexes containing the dichloroacetate moiety in 3-dichoroacetoxylcyclobutane-1,1-dicarboxylate as the leaving group were synthesized, characterized by elemental analysis as well as by ESI+-MS (electrospray ionization mass spectrometry in positive mode), FT-IR, H-1- and C-13-NMR, and evaluated for their in vitro anticancer activity against human lung cancer cell line (A549) and ovarian cancer cell lines (SK-OV-3, SK-OV-3/DDP). Diam(m)ines used in the present study belong to the carriers of six clinically approved platinum drugs. Among the complexes synthesized, complex 2, cis-[Pt(II)(1R,2R-diaminocyclohexane)center dot(3-dichoroacetoxylcyclobutane-1,1-dicarboxylate)] is the most promising in terms of water solubility and potential of being totally devoid of cross-drug resistance with cisplatin. Therefore, complex 2 was selected for the dichloroacetate release test. The test shows dichloroacetate can be efficiently released from complex 2 under physiological conditions via the hydrolysis of an ester bond bridging the dichloroacetate moiety and platinum pharmacophores together. Our study supports the further evaluation of this complex as a drug candidate. (C) 2015 Elsevier Inc. All rights reserved.
资助项目	National Natural Science Foundation of China[21161010] ; Yunnan Provincial Key R&D Program of China[2014BC010]
WOS关键词	ANTITUMOR-ACTIVITY ; CANCER-CHEMOTHERAPY ; TOXICITY ; AGENTS ; DERIVATIVES ; HEPTAPLATIN ; RESISTANCE ; CISPLATIN ; DELIVERY ; PRODRUG
WOS研究方向	Biochemistry & Molecular Biology ; Chemistry
语种	英语
出版者	ELSEVIER SCIENCE INC
WOS记录号	WOS:000353252600002
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276557]
专题	药理学第一研究室
通讯作者	Lou, Liguang
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 2.Kunming Inst Precious Met, State Key Lab Platinum Grp Met, Kunming 650106, Yunnan, Peoples R China;
推荐引用方式 GB/T 7714	Liu, Weiping,Jiang, Jing,Xu, Yongping,et al. Design, synthesis and anticancer activity of diam(m)ine platinum(II) complexes bearing a small-molecular cell apoptosis inducer dichloroacetate[J]. JOURNAL OF INORGANIC BIOCHEMISTRY,2015,146:14-18.
APA	Liu, Weiping.,Jiang, Jing.,Xu, Yongping.,Hou, Shuqian.,Sun, Liping.,...&Lou, Liguang.(2015).Design, synthesis and anticancer activity of diam(m)ine platinum(II) complexes bearing a small-molecular cell apoptosis inducer dichloroacetate.JOURNAL OF INORGANIC BIOCHEMISTRY,146,14-18.
MLA	Liu, Weiping,et al."Design, synthesis and anticancer activity of diam(m)ine platinum(II) complexes bearing a small-molecular cell apoptosis inducer dichloroacetate".JOURNAL OF INORGANIC BIOCHEMISTRY 146(2015):14-18.