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Dithiocarbamic acid esters as anticancer agent. Part 1: 4-substituted-piperazine-1-carbodithioic acid 3-cyano-3,3-diphenyl-propyl esters
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
2006-08-15
DOI10.1016/j.bmcl.2006.05.085
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
引用统计
被引频次:62[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/59940
专题北京大学药学院
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
推荐引用方式
GB/T 7714
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.
APA Hou, Xueling.,Ge, Zemei.,Wang, Tingmin.,Guo, Wei.,Cui, Jingrong.,...&Li, Runtao.(2006).Dithiocarbamic acid esters as anticancer agent. Part 1: 4-substituted-piperazine-1-carbodithioic acid 3-cyano-3,3-diphenyl-propyl esters.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,16(16),4214-4219.
MLA Hou, Xueling,et al."Dithiocarbamic acid esters as anticancer agent. Part 1: 4-substituted-piperazine-1-carbodithioic acid 3-cyano-3,3-diphenyl-propyl esters".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 16.16(2006):4214-4219.
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