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Updated: Sep 24, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and insight into the structure-activity relationships of 2-phenylbenzimidazoles as prospective anticancer
Thi-Kim-Chi Huynh1,2, Thi-Hong-An Nguyen1, Thi-Cam-Thu Nguyen1,3
1Institute of Chemical Technology - VAST 01 Mac Dinh Chi Str., Dist. 1 Ho Chi Minh City Vietnam hoangthikimdung@gmail.com.
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.
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