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

15(1)2025

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

Author - Affiliation:

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

Corresponding author: Bao Le - lebao@tdtu.edu.vn

DOI:10.46223/HCMCOUJS.tech.en.15.1.3580.2025

Submitted: 23-07-2024
Accepted: 27-09-2024
Published: 13-01-2025

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

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Cite this paper as:

Le, T. T., Vu, Y. T., Doan, H. M., & Le, B. (2025). Exploring the anti-cancer potential of coumarin derivatives targeting COX-2 inhibitors. Ho Chi Minh City Open University Journal of Science – Engineering and Technology, 15(1), 28-33. doi:10.46223/HCMCOUJS.tech.en.15.1.3580.2025

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