| Literature DB >> 24576797 |
Ahmed Temirak1, Yasser M Shaker2, Fatma A F Ragab3, Mamdouh M Ali4, Hamed I Ali5, Hoda I El Diwani1.
Abstract
2-(2-Furyl)-1H-benzimidazoles 3-11 were synthesized and tested for their in vitro VEGF inhibition in MCF-7 cancer cell line. Compound 5a was more potent than Tamoxifen, and compounds 3b, 5a, 5c, 6b, 7a and 10 showed promising potency. Furthermore, compounds (6b, 7a and 10) showed remarkable selective inhibition of COX-2 enzyme close to that of Celecoxcib. Additionally, docking studies were performed using AutoDock 4.2 into the VEGFR2 kinase. Significant correlation exists between the biological activity (IC50 and %VEGF inhibition) against MCF-7 cell line and the molecular docking results (Ki and ΔGb) with correlation coefficients (R(2)) of 0.5513 and 0.4623 respectively. Accordingly, most of the synthesized 2-(2-furyl)-1H-benzimidazoles showed strong antiangiogenic activity against VEGFR2 kinase.Entities:
Keywords: 2-(2-Furyl)-1H-benzimidazoles; Angiogenesis; Cytotoxicity; VEGFR2 kinase; Vascular endothelial growth factor (VEGF)
Mesh：
Substances：
Year: 2014 PMID： 24576797 DOI： 10.1016/j.ejmech.2014.01.063
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514