Synthesis, biological evaluation, and docking studies of new 2-furylbenzimidazoles as anti-angiogenic agents: part II. Academic Article uri icon


  • The 2-(5-methyl-2-furyl)-1H-benzimidazole moiety has shown promising activity against vascular endothelial growth factor (VEGF)-induced angiogenesis. In part I of this study, we have synthesized new analogs and tested their anti-angiogenic potentials. Here, we continue our previous study with different new analogs. Some compounds show promising cytotoxic activity against the human breast cancer cell line MCF-7, with IC50 in the range of 7.80-13.90g/mL, and exhibited remarkable in vitro inhibition against VEGF in the MCF-7 cancer cell line, with 95-98% of inhibition in comparison to tamoxifen as reference (IC50: 8.00g/mL, % of inhibition=98%). Additionally, a molecular docking study was carried out to gain insight into plausible binding modes and to understand the structure-activity relationships of the synthesized compounds.

published proceedings

  • Arch Pharm (Weinheim)

author list (cited authors)

  • Temirak, A., Shaker, Y. M., Ragab, F., Ali, M. M., Soliman, S. M., Mortier, J., ... El Diwani, H. I.

citation count

  • 16

complete list of authors

  • Temirak, Ahmed||Shaker, Yasser M||Ragab, Fatma AF||Ali, Mamdouh M||Soliman, Salwa M||Mortier, Jeremie||Wolber, Gerhard||Ali, Hamed I||El Diwani, Hoda I

publication date

  • April 2014