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Ibrahim H. Eissa Radwan El-Haggar Mohammed A. Dahab Marwa F. Ahmed Hazem A. Mahdy Reem I. Alsantali Alaa Elwan Nicolas Masurier Samar S. Fatahala 《Journal of enzyme inhibition and medicinal chemistry》2022,37(1):1587
A novel series of 2-thioacetamide linked benzoxazole-benzamide conjugates 1–15 was designed as potential inhibitors of the vascular endothelial growth factor receptor-2 (VEGFR-2). The prepared compounds were evaluated for their potential antitumor activity and their corresponding selective cytotoxicity was estimated using normal human fibroblast (WI-38) cells. Compounds 1, 9–12 and 15 showed good selectivity and displayed excellent cytotoxic activity against both HCT-116 and MCF-7 cancer cell lines compared to sorafenib, used as a reference compound. Furthermore, compounds 1 and 11 showed potent VEGFR-2 inhibitory activity. The cell cycle progression assay showed that 1 and 11 induced cell cycle arrest at G2/M phase, with a concomitant increase in the pre-G1 cell population. Further pharmacological studies showed that 1 and 11 induced apoptosis and inhibited the expression of the anti-apoptotic Bcl-2 and Bcl-xL proteins in both cell lines. Therefore, compounds 1 and 11 might serve as promising candidates for future anticancer therapy development. 相似文献
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Xiaopeng Sun Belal Amany Elanany Mohamed A. Alsantali Reem I. Alrooqi Munira M. Mohamed Abdalla R. Hasabelnaby Sherifa 《Russian Journal of Bioorganic Chemistry》2022,48(2):438-456
Russian Journal of Bioorganic Chemistry - Rhinitis is an allergic disease that causes troubles and restlessness for patients. In this research work we will focus on finding promising organic... 相似文献
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