Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives

被引：9

作者：

Zhai Xin ^{[1
]}

He Ying ^{[1
]}

Yang Zhen ^{[1
]}

Gong Ping ^{[1
]}

机构：

[1] Shenyang Pharmaceut Univ, Key Lab Struct Based Drug Design & Discovery, Minist Educ, Sch Pharmaceut Engn, Shenyang 110016, Peoples R China

来源：

CHEMICAL RESEARCH IN CHINESE UNIVERSITIES | 2013年 / 29卷 / 01期

基金：

中国国家自然科学基金;

关键词：

Thiosemicarbazide; N-methylpicolinamide; Antiproliferative activity; DESIGN; BENZIMIDAZOLES; CYTOTOXICITY;

D O I：

10.1007/s40242-013-2136-5

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of novel N-methylpicolinamide-moiety containing diarylthiosemicarbazide derivatives was prepared and evaluated for their in vitro antiproliferative activity against three cancer cell lines(human alveolar epithelial cell A549, human lung cancer cell 11460 and human colorectal cancer cell HT-29) by 3-(4,5-dimethyl)thiazolyl-diphenyltetrazoliumromide(MTT) assay. Six compounds(7b-7g) with halogen substituents exhibited preferable cytotoxicity against one or more cell lines in a low micromolar range. Especially, the most promising compound 7g exhibited remarkable antiproliferative activity with the IC50 values of 2.2, 1.8 and 5.2 mu mol/L against A549, 11460 and HT-29 cell lines respectively, which is comparable to sorafenib.

引用

页码：62 / 66

页数：5

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