Synthesis and biological activity evaluation of coumarin-3-carboxamide derivatives

28Citations
Citations of this article
39Readers
Mendeley users who have this article in their library.

Abstract

A series of novel coumarin-3-carboxamide derivatives were designed and synthesized to evaluate their biological activities. The compounds showed little to no activity against gram-positive and gram-negative bacteria but specifically showed potential to inhibit the growth of cancer cells. In particular, among the tested compounds, 4-fluoro and 2,5-difluoro benzamide derivatives (14b and 14e, respectively) were found to be the most potent derivatives against HepG2 cancer cell lines (IC50 = 2.62–4.85 µM) and HeLa cancer cell lines (IC50 = 0.39–0.75 µM). The activities of these two compounds were comparable to that of the positive control doxorubicin; especially, 4-flurobenzamide derivative (14b) exhibited low cytotoxic activity against LLC-MK2 normal cell lines, with IC50 more than 100 µM. The molecular docking study of the synthesized compounds revealed the binding to the active site of the CK2 enzyme, indicating that the presence of the benzamide functionality is an important feature for anticancer activity.

Cite

CITATION STYLE

APA

Phutdhawong, W., Chuenchid, A., Taechowisan, T., Sirirak, J., & Phutdhawong, W. S. (2021). Synthesis and biological activity evaluation of coumarin-3-carboxamide derivatives. Molecules, 26(6). https://doi.org/10.3390/molecules26061653

Register to see more suggestions

Mendeley helps you to discover research relevant for your work.

Already have an account?

Save time finding and organizing research with Mendeley

Sign up for free