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

作者：Bao, Guanglong; Du, Baoquan; Ma, Yuxiu; Zhao, Meng; Gong, Ping; Zhai, Xin^*

来源：Medicinal Chemistry, 2016, 12(5): 489-498.

DOI：10.2174/1573406412666160107113343

• Benzothiazole
• semicarbazone
• synthesis
• antiproliferative activity

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.

• 出版日期2016
• 单位沈阳药科大学