Exploring the anti-cancer potential of coumarin derivatives targeting COX-2 inhibitors

Thanh Tin Le; Y Thien Vu; Hieu Minh Doan; Bao Le

doi:10.46223/HCMCOUJS.tech.en.15.1.3580.2025

Authors

Thanh Tin Le
Ho Chi Minh City University of Education, Ho Chi Minh City
Y Thien Vu
Ton Duc Thang University, Ho Chi Minh City
Hieu Minh Doan
Ton Duc Thang University, Ho Chi Minh City
Bao Le lebao@tdtu.edu.vn
Ton Duc Thang University, Ho Chi Minh City

DOI:

https://doi.org/10.46223/HCMCOUJS.tech.en.15.1.3580.2025

Keywords:

anti-cancer, coumarin, COX-2 inhibitors, synthesis

Abstract

Overexpression of cyclooxygenase-2 (COX-2) plays a crucial role in cancer therapy. In this study, we investigated the role of two coumarin derivatives with the chlorobenzylamide group in inhibiting COX-2 activity and growth inhibition of cancer cells. The effect of synthesized 2a and 2b coumarin derivatives on COX-2 enzyme was investigated in vitro. Besides that, A549, HT-29, MDA-MMB-231, and HeLa tumor cell lines were used to evaluate potential inhibition growth using the MTT assay. According to the results, two synthesized compounds showed an inhibitory effect on COX-2 enzymes. In particular, 2a exhibited the best activity with an IC50 value of 49.54μM on COX-2. The 2a and 2b exhibited a noteworthy dose-dependent inhibitory growth activity against all the tested cancer cell lines, indicating their broad-spectrum anti-cancer properties. Based on the in vitro data, we strongly recommend this new coumarin-o-chlorobenzylamide as a preclinical development candidate for novel anti-cancer agents targeting COX-2 inhibition.

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