دورية أكاديمية
Development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer
| العنوان: | Development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer |
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| المؤلفون: | Wagdy M. Eldehna, Rofaida Salem, Zainab M. Elsayed, Tarfah Al-Warhi, Hamada R. Knany, Rezk R. Ayyad, Thamer Bin Traiki, Maha-Hamadien Abdulla, Rehan Ahmad, Hatem A. Abdel-Aziz, Radwan El-Haggar |
| المصدر: | Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 36, Iss 1, Pp 1423-1434 (2021) |
| بيانات النشر: | Taylor & Francis Group, 2021. |
| سنة النشر: | 2021 |
| المجموعة: | LCC:Therapeutics. Pharmacology |
| مصطلحات موضوعية: | benzofuran hydrazide, isatin, cleaved parp, bcl2 inhibitors, colon cancer, Therapeutics. Pharmacology, RM1-950 |
| الوصف: | In the current work, a new set of carbohydrazide linked benzofuran-isatin conjugates (5a–e and 7a–i) was designed and synthesised. The anticancer activity for compounds (5b–d, 7a, 7b, 7d and 7g) was measured against NCI-55 human cancer cell lines. Compound 5d was the most efficient, and thus subjected to the five-dose screen where it showed excellent broad activity against almost all tested cancer subpanels. Furthermore, all conjugates (5a–e and 7a–i) showed a good anti-proliferative activity towards colorectal cancer SW-620 and HT-29 cell lines, with an excellent inhibitory effect for compounds 5a and 5d (IC50 = 8.7 and 9.4 µM (5a), and 6.5 and 9.8 µM for (5d), respectively). Both compounds displayed selective cytotoxicity with good safety profile. In addition, both compounds provoked apoptosis in a dose dependent manner in SW-620 cells. Also, they significantly inhibited the anti-apoptotic Bcl2 protein expression and increased the cleaved PARP level that resulted in SW-620 cells apoptosis. |
| نوع الوثيقة: | article |
| وصف الملف: | electronic resource |
| اللغة: | English |
| تدمد: | 1475-6366 1475-6374 14756366 |
| Relation: | https://doaj.org/toc/1475-6366; https://doaj.org/toc/1475-6374 |
| DOI: | 10.1080/14756366.2021.1944127 |
| URL الوصول: | https://doaj.org/article/3772b97f90654613a38cd0678b5d84ab |
| رقم الأكسشن: | edsdoj.3772b97f90654613a38cd0678b5d84ab |
| قاعدة البيانات: | Directory of Open Access Journals |
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Full Text Finder | تدمد: | 14756366 14756374 |
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| DOI: | 10.1080/14756366.2021.1944127 |