Synthesis and biological evaluation of 2-(3-aminophenyl)-benzothiazoles as antiproliferative and apoptosis-inducing agents
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A series of new 2-(3-aminophenyl)-benzothiazole derivatives were synthesized and evaluated for their in vitro antiproliferative activity against various human cancer cell lines including A549, HeLa, HepG2, MCF-7, MV4-11, and DB. Among the tested compounds, N-[3-(benzo[d]thiazol-2-yl)phenyl]nicotinamide displayed significantly improved antiproliferative activity toward A549 and MV4-11 cells with IC50 values of 5.42 ± 1.33 and 7.51 ± 0.98 μM, respectively, much stronger than the hit 3-(benzo[d]thiazol-2-yl)-N-(4-bromobenzyl)aniline. Furthermore, flow cytometric analysis indicated that N-[3-(benzo[d]thiazol-2-yl)phenyl]nicotinamide induced A549 cell apoptosis with cell cycle arrest at G1 phase in a concentration-dependent manner.
KeywordsHeterocycles Cytotoxicity Antitumor agents Cell cycle arrest Structure–activity relationships
This research work was financially supported by the National Natural Science Foundation of China (No. 21672082), Shandong Key Development Project (No. 2016GSF201209), the Young Taishan Scholars Program (No. tsqn20161037), Natural Science Foundation of Shandong Province (Nos. ZR2017BH038, JQ201721), Shandong Talents Team Cultivation Plan of University Preponderant Discipline (No. 10027), and the Brazilian Government Agencies FAP/DF and CNPq.
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