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Date Published: 30/09/2024
Online Published: 30/09/2024
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DOI: https://doi.org/10.54607/hcmue.js.21.9.4241(2024)
Issue
Vol. 21 No. 9 (2024)
Section
Articles
How to Cite
Lê , T. T., Đoàn , M. H., Nguyễn , T. T. T., Lê , T. T. H., Vũ , T. Ý., Nguyễn , P. H., & Đức , D. V. (2024). SYNTHESIS OF NEW COUMARIN DERIVATIVES AND EVALUATION OF THEIR ANTI-CANCER ACTIVITY. HCMUE Journal of Science, 21(9), 1682. https://doi.org/10.54607/hcmue.js.21.9.4241(2024)

SYNTHESIS OF NEW COUMARIN DERIVATIVES AND EVALUATION OF THEIR ANTI-CANCER ACTIVITY

Tín Thanh Lê 1, , Minh Hiếu Đoàn , Thị Thu Trang Nguyễn , Thị Thanh Hương Lê , Thiên Ý Vũ , Phú Hùng Nguyễn , Duy Võ Đức
1 Faculty of Chemistry, Ho Chi Minh City University of Education

Main Article Content

Abstract

A fragment-based approach has been applied to derive 2-(7-hydroxy-2-oxo-2H-chromen-4-yl)acetic acid 1 into 4 new coumarin derivatives 2a-d through amide bonds. The compounds were screened for their anticancer activity using MTT assay on MCF-7 and HepG2 cell lines. The results showed that compounds 2a-c significantly inhibited MCF-7 cells at 40 µM (29-38%) while compound 2d is a strong HepG2 inhibitor with IC50 of 21 µM. Docking studies of the most potent compound 2d suggest its HepG2 antiproliferative activity could be mediated through multikinase inhibition of p38α, VEGFR2 and FGFR-1. Further optimisation should lead to a more potent compound.

 

 

Keywords

2-(7-hydroxy-2-oxo-2H-chromen-4-yl)acetic acid, amide coupling, anticancer, MCF-7, HepG2, molecular docking

Article Details

References

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