Abstract

Weerachai Phutdhawong¹, Sopita Rattanopas², Jitnapa Sirirak², Thongchai Taechowisan³ and Waya S. Phutdhawong*²

DOI : http://dx.doi.org/10.13005/ojc/350231

Azepinobisindole derivatives, the isomeric Iheyamine skeleton, was prepared and its anticancer activity evaluation were investigated against two human cancer cell lines, Hepatocellular carcinoma (HepG2) and human cervical cancer line (Hela) as well as the normal cell line (Vero cell line) using MTT assay. The anticancer activity results indicated that 2-methoxy-5-methyl-5H-azepino[2,3-b:4,5-bʹ]diindole was the most active derivative against tested cell lines.  Additionally, molecular docking study in silico the possible inhibitory effect of cyclin-dependent kinase 2 (CDK2) by the azepinoindole revealed that all synthesized compounds fit well in the binding cavity of CDK2.

Anticancer Activity; Azepinobisindole; CDK2; Isomeric Iheyamine; Molecular Docking

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