Exploring the anti-cancer potential of coumarin derivatives targeting COX-2 inhibitors
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 der...
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| Format: | Article |
| Language: | English |
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HO CHI MINH CITY OPEN UNIVERSITY JOURNAL OF SCIENCE
2025-01-01
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| Series: | Ho Chi Minh City Open University Journal of Science - Engineering and Technology |
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| Online Access: | https://journalofscience.ou.edu.vn/index.php/tech-en/article/view/3580 |
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| _version_ | 1850187659996037120 |
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| author | Thanh Tin Le Y Thien Vu Hieu Minh Doan Bao Le |
| author_facet | Thanh Tin Le Y Thien Vu Hieu Minh Doan Bao Le |
| author_sort | Thanh Tin Le |
| collection | DOAJ |
| description | 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. |
| format | Article |
| id | doaj-art-d8d56066073a405097a6e875fbcddff1 |
| institution | OA Journals |
| issn | 2734-9330 2734-9608 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | HO CHI MINH CITY OPEN UNIVERSITY JOURNAL OF SCIENCE |
| record_format | Article |
| series | Ho Chi Minh City Open University Journal of Science - Engineering and Technology |
| spelling | doaj-art-d8d56066073a405097a6e875fbcddff12025-08-20T02:16:04ZengHO CHI MINH CITY OPEN UNIVERSITY JOURNAL OF SCIENCEHo Chi Minh City Open University Journal of Science - Engineering and Technology2734-93302734-96082025-01-01151283310.46223/HCMCOUJS.tech.en.15.1.3580.20252336Exploring the anti-cancer potential of coumarin derivatives targeting COX-2 inhibitorsThanh Tin Le0Y Thien Vu1Hieu Minh Doan2Bao Le3Ho Chi Minh City University of Education, Ho Chi Minh CityTon Duc Thang University, Ho Chi Minh CityTon Duc Thang University, Ho Chi Minh CityTon Duc Thang University, Ho Chi Minh CityOverexpression 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.https://journalofscience.ou.edu.vn/index.php/tech-en/article/view/3580anti-cancercoumarincox-2 inhibitorssynthesis |
| spellingShingle | Thanh Tin Le Y Thien Vu Hieu Minh Doan Bao Le Exploring the anti-cancer potential of coumarin derivatives targeting COX-2 inhibitors Ho Chi Minh City Open University Journal of Science - Engineering and Technology anti-cancer coumarin cox-2 inhibitors synthesis |
| title | Exploring the anti-cancer potential of coumarin derivatives targeting COX-2 inhibitors |
| title_full | Exploring the anti-cancer potential of coumarin derivatives targeting COX-2 inhibitors |
| title_fullStr | Exploring the anti-cancer potential of coumarin derivatives targeting COX-2 inhibitors |
| title_full_unstemmed | Exploring the anti-cancer potential of coumarin derivatives targeting COX-2 inhibitors |
| title_short | Exploring the anti-cancer potential of coumarin derivatives targeting COX-2 inhibitors |
| title_sort | exploring the anti cancer potential of coumarin derivatives targeting cox 2 inhibitors |
| topic | anti-cancer coumarin cox-2 inhibitors synthesis |
| url | https://journalofscience.ou.edu.vn/index.php/tech-en/article/view/3580 |
| work_keys_str_mv | AT thanhtinle exploringtheanticancerpotentialofcoumarinderivativestargetingcox2inhibitors AT ythienvu exploringtheanticancerpotentialofcoumarinderivativestargetingcox2inhibitors AT hieuminhdoan exploringtheanticancerpotentialofcoumarinderivativestargetingcox2inhibitors AT baole exploringtheanticancerpotentialofcoumarinderivativestargetingcox2inhibitors |