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

Thanh Tin Le, Y Thien Vu, Hieu Minh Doan and Bao Le ()
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Thanh Tin Le: Ho Chi Minh City University of Education, Ho Chi Minh City, Vietnam
Y Thien Vu: Ton Duc Thang University, Ho Chi Minh City, Vietnam
Hieu Minh Doan: Ton Duc Thang University, Ho Chi Minh City, Vietnam
Bao Le: Ton Duc Thang University, Ho Chi Minh City, Vietnam

HO CHI MINH CITY OPEN UNIVERSITY JOURNAL OF SCIENCE - ENGINEERING AND TECHNOLOGY, 2025, vol. 15, issue 1, 28-33

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.

Keywords: anti-cancer; coumarin; COX-2 inhibitors; synthesis (search for similar items in EconPapers)
Date: 2025
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Persistent link: https://EconPapers.repec.org/RePEc:bjw:techen:v:15:y:2025:i:1:p:28-33

DOI: 10.46223/HCMCOUJS.tech.en.15.1.3580.2025

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