2. Academic Validation
  3. Part I. Synthesis, biological evaluation and docking studies of new 2-furylbenzimidazoles as antiangiogenic agents

Part I. Synthesis, biological evaluation and docking studies of new 2-furylbenzimidazoles as antiangiogenic agents

  • Eur J Med Chem. 2014 Nov 24:87:868-80. doi: 10.1016/j.ejmech.2014.01.063.
Ahmed Temirak 1,  Yasser M Shaker 2,  Fatma A F Ragab 3,  Mamdouh M Ali 4,  Hamed I Ali 5,  Hoda I El Diwani 1
Affiliations

Affiliations

  • 1 Department of Chemistry of Natural and Microbial Products, Division of Pharmaceutical and Drug Industries, National Research Centre, Dokki, 12622 Cairo, Egypt.
  • 2 Department of Chemistry of Natural and Microbial Products, Division of Pharmaceutical and Drug Industries, National Research Centre, Dokki, 12622 Cairo, Egypt. Electronic address: yabdelrahman@yahoo.com.
  • 3 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Cairo University, Egypt.
  • 4 Department of Biochemistry, Division of Genetic Engineering and Biotechnology, National Research Centre, 12622 Cairo, Egypt.
  • 5 Department of Pharmaceutical Sciences, Irma Lerma Rangel College of Pharmacy, Texas A&M Health Science Center, TX, USA; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Helwan University, Cairo, Egypt.
PMID: 24576797 DOI: 10.1016/j.ejmech.2014.01.063
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/KDR/Flk-1 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/KDR/Flk-1 kinase.

Keywords

2-(2-Furyl)-1H-benzimidazoles; Angiogenesis; Cytotoxicity; VEGFR2 kinase; Vascular endothelial growth factor (VEGF).

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