Design, Synthesis and Antiproliferative Activity of Novel Benzothiazole Derivatives Conjugated with Semicarbazone Scaffold

被引：5

作者：

Bao, Guanglong ^{[1
]}

Du, Baoquan ^{[1
]}

Ma, Yuxiu ^{[2
]}

Zhao, Meng ^{[1
]}

Gong, Ping ^{[1
]}

Zhai, Xin ^{[1
]}

机构：

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

[2] CSPC Zhongqi Pharmaceut Technol Shijiazhuang Co L, Shijiazhuang 050001, Peoples R China

来源：

MEDICINAL CHEMISTRY | 2016年 / 12卷 / 05期

基金：

中国国家自然科学基金;

关键词：

Benzothiazole; semicarbazone; synthesis; antiproliferative activity; BIOLOGICAL EVALUATION; ANTITUMOR; BEARING; POTENT; OPTIMIZATION; DISCOVERY; MOIETY;

D O I：

10.2174/1573406412666160107113343

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Two series of novel benzothiazole derivatives conjugated with semicarbazone scaffold were designed and synthesized through a structure-based molecular hybridization strategy. All the target compounds were evaluated for their cytotoxicity in vitro against three cancer cell lines (HT-29, MKN-45 and H460) by standard MTT assay. The pharmacological results indicated that seven compounds (17h-n) exhibited comparable or even better antiproliferative activity in comparison with reference drugs Sorafenib and PAC-1. Particularly, compound 17i displayed remarkable cytotoxicity against tested three cancer cell lines with IC50 values of 0.84, 0.06 and 0.52 mu M, which were 4.3-, 36.6-, 4.2-folds more potent than Sorafenib and 1.2-, 13.7-, 6.9-times more active than PAC-1, respectively.

引用

页码：489 / 498

页数：10

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