Issue 35, 2020, Issue in Progress

Synthesis and insight into the structure–activity relationships of 2-phenylbenzimidazoles as prospective anticancer agents

Abstract

In order to explore and develop new anticancer agents, three series of 2-phenylbenzimidazoles, 15–46, were condensed under simple and mild conditions using sodium metabisulfite as an oxidation agent and another series, 47–55, were obtained via a reduction reaction using sodium borohydride. All the compounds synthesized were evaluated for their in vitro anticancer activities against three human cancer cell lines. The novel compound 38 was found to be the most potent multi cancer inhibitor against A549, MDA-MB-231, and PC3 cell lines (IC50 values 4.47, 4.68 and 5.50 μg mL−1, respectively). In addition, compound 40 exhibited the best IC50 value of 3.55 μg mL−1 against the MDA-MB-231 cell line. The results demonstrated that introducing a new substituent to compounds 37–55 could improve their antiproliferative activities.

Graphical abstract: Synthesis and insight into the structure–activity relationships of 2-phenylbenzimidazoles as prospective anticancer agents

Supplementary files

Article information

Article type
Paper
Submitted
11 Mar 2020
Accepted
10 May 2020
First published
01 Jun 2020
This article is Open Access
Creative Commons BY-NC license

RSC Adv., 2020,10, 20543-20551

Synthesis and insight into the structure–activity relationships of 2-phenylbenzimidazoles as prospective anticancer agents

T. Huynh, T. Nguyen, T. Nguyen and T. Hoang, RSC Adv., 2020, 10, 20543 DOI: 10.1039/D0RA02282A

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