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学科主题: Pharmacology & Pharmacy ; Chemistry
题名: Synthesis and Structure-Activity Relationships of A Novel Class of Dithiocarbamic Acid Esters as Anticancer Agent
作者: Hou Xueling; Ge Zemei; Wang Tingmin; Guo Wei; Wu Jun; Cui Jingrong; Lai Chingsan; Li Runtao
关键词: Anticancer activity ; Dithiocarbamic acid ester ; Dithiocarbamic acid ester ; SARs ; SARs
刊名: ARCHIV DER PHARMAZIE
发表日期: 2011
DOI: 10.1002/ardp.201000259
卷: 344, 期:5, 页:320-332
收录类别: SCI
资助者: Natural Science Foundation of China NSFC 20672009
摘要: Based on a novel lead compound 4-methylpiperazine-1-carbodithioic acid 3-cyano-3,3-diphenylpropyl ester 1, the systematic structural modification was carried out. All the synthesized compounds were evaluated for their in-vitro anticancer activities on four to six different cell lines at three different concentrations. Most of the tested compounds could selectively inhibit the growth of HL-60 and Bel-7402 cell lines at a medium concentration. Four compounds (3f, 3g, 3n, and 5) were selected for the IC(50) test, and the results revealed that three compounds (3g, 3n, and 5) showed almost the same or a slightly weaker activity than compound 1 against HL-60, and three compounds (3f, 3g, and 3n) showed > 2-fold higher potency than compound 1 against Bel-7402. The in-vivo efficacy of 3n center dot HCl was evaluated with transplanted hepatocyte carcinoma 22 as an in-vivo test model. It was found that 3n center dot HCl could inhibit significantly the growth of tumor, and that this effect was dose-dependent. Meanwhile, the compound 3n center dot HCl showed low toxicity compared with compound 1 center dot HCl as evidenced by the little body-weight loss. These results confirmed that compound 3n center dot HCl is more potent than the lead compound 1 center dot HCl. Preliminary structure-activity relationships indicated that: a) Both nitrile group and the cyclic amine containing at least two nitrogens were indispensable moieties to keep the activity; b) substitution of the piperazine ring is unfavorable for the improvement of activity; c) the suitable linker joining the piperazinyl dithiocarboxyl and diphenylacetonitril group should be ethylene; d) a non-coplanar arrangement of the two benzene rings appears to be essential for activity.
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内容类型: 期刊论文
URI标识: http://ir.xjipc.cas.cn/handle/365002/1663
Appears in Collections:新疆维吾尔自治区植物资源化学重点实验室 _期刊论文

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作者单位: Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China;Medinox Inc, San Diego, CA USA;Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, Key Lab Chem Plant Resources Arid Area, Urumqi, Peoples R China

Recommended Citation:
Hou Xueling,Ge Zemei,Wang Tingmin,et al. Synthesis and Structure-Activity Relationships of A Novel Class of Dithiocarbamic Acid Esters as Anticancer Agent[J]. ARCHIV DER PHARMAZIE,2011,344(5):320-332.
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