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学科主题: 药学
题名:
Dithiocarbamic acid esters as anticancer agent. Part 1: 4-substituted-piperazine-1-carbodithioic acid 3-cyano-3,3-diphenyl-propyl esters
作者: Hou, Xueling; Ge, Zemei; Wang, Tingmin; Guo, Wei; Cui, Jingrong; Cheng, Tieming; Lai, Chingshan; Li, Runtao
关键词: dithiocarbamic acid ester ; anticancer activity ; 4-substituted-piperazine-1-carbodithioic acid 3-cyano-3,3-diphenyl-propyl ester ; synthesis
刊名: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
发表日期: 2006-08-15
DOI: 10.1016/j.bmcl.2006.05.085
卷: 16, 期:16, 页:4214-4219
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal ; Chemistry, Organic
研究领域[WOS]: Pharmacology & Pharmacy ; Chemistry
关键词[WOS]: IN-VITRO ; NEPHROTOXICITY ; PLATINUM(II) ; DERIVATIVES ; ASSAY
英文摘要:

A variety of 4-N atom substituted derivatives were synthesized and evaluated for their in vitro anticancer activities using 4-methylpiperazine-1-carbodithioic acid 3-cyano-3,3-diphenyl-propyl ester 4 as lead compound. Among them, compound 6a without any substituent on 4-N atom (R-1 = H) was found to be the most active anticancer agent with IC50 = 5.3 mu M against HL-60 and IC50 = 11.5 mu M against Bel-7402, respectively. Increase in the polarity and/or introduction of suitable acyl groups at the 4-N atom of the lead compound 4 are favorable for the improvement of activity. (c) 2006 Elsevier Ltd. All rights reserved.

语种: 英语
WOS记录号: WOS:000239349000011
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/59940
Appears in Collections:北京大学药学院_期刊论文

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作者单位: 1.Medinox Inc, San Diego, CA 92121 USA
2.Peking Univ, Sch Pharmaceut Sci, Beijing 100083, Peoples R China
3.Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100083, Peoples R China

Recommended Citation:
Hou, Xueling,Ge, Zemei,Wang, Tingmin,et al. Dithiocarbamic acid esters as anticancer agent. Part 1: 4-substituted-piperazine-1-carbodithioic acid 3-cyano-3,3-diphenyl-propyl esters[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2006,16(16):4214-4219.
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