Synthesis and Anticancer Activity of cis-[Pt(II)(trans-1,2-bis(methylamino)cyclobutane) (3-hydroxyl-1,1-cyclobutanedicarboxylate)]

doi:10.11862/CJIC.2017.096

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药理学第一研究室

	Synthesis and Anticancer Activity of cis-[Pt(II)(trans-1,2-bis(methylamino)cyclobutane) (3-hydroxyl-1,1-cyclobutanedicarboxylate)]
	Gao An-Li 1; Qiu Jie 3; Hou Shu-Qian 1; Jiang Jing 1; Lou Li-Guang2 ; Liu Wei-Ping 1
刊名	CHINESE JOURNAL OF INORGANIC CHEMISTRY
	2017-05-10
卷号	33 期号:5 页码:837-842
关键词	platinum complexes synthesis characterization anticancer activity
ISSN号	1001-4861
DOI	10.11862/CJIC.2017.096
文献子类	Article
英文摘要	A new water-soluble and more water-stable analogue of lobaplatin, cis-[Pt(II)(trans-1,2-bis(methylamino) cyclobutane)(3-hydroxyl-1,1-cyclobutanedicarboxylate)], was designed, with an attempt to improve the water-stability of lobaplatin while retaining its excellent anticancer profile, via the structural recombination and optimization of lobaplatin and carboplatin. The analogue was synthesized by the direct reaction between cis-[Pt(II)(trans-1,2-bis (methylamino))I-2 as an intermediate and the silver salt of 3-hydroxyl-1,1-cyclobutanedicarboxylic acid, and characterized by elemental analysis, ESI-MS, IR and H-1, C-13 NMR. The anticancer activity was evaluated by both in vitro cyotoxicity against four human cancer cell lines and in vivo antitumor efficiency in human lung carcinoma NCI-H460 xenografts in nude mice. The biological tests revealed that the analogue produced significant inhibition of the tumor growth, resulting in an inhibitory rate of 54% at the dose of 60 mg.kg (-1) and more importantly, it had in vivo anticancer activity comparable to that of lobaplatin.
WOS关键词	PLATINUM COMPLEXES ; ANTITUMOR-ACTIVITY ; ANALOG ; HEPTAPLATIN ; TOXICITY ; DELIVERY ; AGENTS ; DRUGS
WOS研究方向	Chemistry
语种	中文
CSCD记录号	CSCD:5987271
出版者	CHINESE CHEMICAL SOC
WOS记录号	WOS:000405542200015
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/272666]
专题	药理学第一研究室
通讯作者	Jiang Jing; Liu Wei-Ping
作者单位	1.Kunming Inst Precious Met, Platinum Based Drug Lab, Kunming 650106, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Tumor PharmacologyLab, Shanghai 201203, Peoples R China 3.Lincang Maternal & Child Hlth Care Hosp, Lincang 677000, Yunnan, Peoples R China;
推荐引用方式 GB/T 7714	Gao An-Li,Qiu Jie,Hou Shu-Qian,et al. Synthesis and Anticancer Activity of cis-[Pt(II)(trans-1,2-bis(methylamino)cyclobutane) (3-hydroxyl-1,1-cyclobutanedicarboxylate)][J]. CHINESE JOURNAL OF INORGANIC CHEMISTRY,2017,33(5):837-842.
APA	Gao An-Li,Qiu Jie,Hou Shu-Qian,Jiang Jing,Lou Li-Guang,&Liu Wei-Ping.(2017).Synthesis and Anticancer Activity of cis-[Pt(II)(trans-1,2-bis(methylamino)cyclobutane) (3-hydroxyl-1,1-cyclobutanedicarboxylate)].CHINESE JOURNAL OF INORGANIC CHEMISTRY,33(5),837-842.
MLA	Gao An-Li,et al."Synthesis and Anticancer Activity of cis-[Pt(II)(trans-1,2-bis(methylamino)cyclobutane) (3-hydroxyl-1,1-cyclobutanedicarboxylate)]".CHINESE JOURNAL OF INORGANIC CHEMISTRY 33.5(2017):837-842.