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

Author

Listed:
  • 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)

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.

Suggested Citation

  • Thanh Tin Le & Y Thien Vu & Hieu Minh Doan & Bao Le, 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, HO CHI MINH CITY OPEN UNIVERSITY JOURNAL OF SCIENCE, HO CHI MINH CITY OPEN UNIVERSITY, vol. 15(1), pages 28-33.
    • Handle: 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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