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

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

Volume: 12 Issue: 5

Author(s): Guanglong Bao, Baoquan Du, Yuxiu Ma, Meng Zhao, Ping Gong and Xin Zhai

Affiliation:

Keywords: Benzothiazole, semicarbazone, synthesis, antiproliferative activity.

Abstract: 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 µM, 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.

Cite this article as:

Bao Guanglong, Du Baoquan, Ma Yuxiu, Zhao Meng, Gong Ping and Zhai Xin, Design, Synthesis and Antiproliferative Activity of Novel Benzothiazole Derivatives Conjugated with Semicarbazone Scaffold, Medicinal Chemistry 2016; 12 (5) . https://dx.doi.org/10.2174/1573406412666160107113343