Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives

doi:10.1007/s40242-013-2136-5

高等学校化学研究 ›› 2013, Vol. 29 ›› Issue (1): 62-66.doi: 10.1007/s40242-013-2136-5

Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives

ZHAI Xin, HE Ying, YANG Zhen, GONG Ping

Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China

收稿日期:2012-04-05 修回日期:2012-05-15 出版日期:2013-02-01 发布日期:2013-01-23
基金资助:
Supported by the National Natural Science Foundation of China(No.21002065) and the Science & Technology Project of Liaoning Province, China(No.LJQ201107).

Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives

ZHAI Xin, HE Ying, YANG Zhen, GONG Ping

Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China

Received:2012-04-05 Revised:2012-05-15 Online:2013-02-01 Published:2013-01-23
Supported by:
Supported by the National Natural Science Foundation of China(No.21002065) and the Science & Technology Project of Liaoning Province, China(No.LJQ201107).

摘要/Abstract

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 H460 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 IC₅₀values of 2.2, 1.8 and 5.2 μmol/L against A549, H460 and HT-29 cell lines respectively, which is comparable to sorafenib.

关键词: Thiosemicarbazide, N-methylpicolinamide, Antiproliferative activity

Abstract:

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 H460 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 μmol/L against A549, H460 and HT-29 cell lines respectively, which is comparable to sorafenib.

Key words:

Thiosemicarbazide, N-methylpicolinamide, Antiproliferative activity

ZHAI Xin, HE Ying, YANG Zhen, GONG Ping. Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives[J]. 高等学校化学研究, 2013, 29(1): 62-66.

ZHAI Xin, HE Ying, YANG Zhen, GONG Ping. Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives[J]. Chemical Research in Chinese Universities, 2013, 29(1): 62-66.

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Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives

Syntheses and Antiproliferative Activities of Novel Diarylthiosemicarbazide Derivatives

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