Synthesis, biological evaluation, and docking studies of new 2-furylbenzimidazoles as anti-angiogenic agents: part II.
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 7.80-13.90 µg/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: 8.00 µg/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.
Division of Pharmaceutical and Drug Industries, Department of Chemistry of Natural and Microbial Products, National Research Center, Dokki, Cairo, Egypt.
Ahmed
A
Temirak
Yasser M
YM
Shaker
Fatma A F
FA
Ragab
Mamdouh M
MM
Ali
Salwa M
SM
Soliman
Jeremie
J
Mortier
Gerhard
G
Wolber
Hamed I
HI
Ali
Hoda I
HI
El Diwani
D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000098:blood supply / Q000188:drug therapy*; D005260:Female; D006801:Humans; D020128:Inhibitory Concentration 50; D061986:MCF-7 Cells; D062105:Molecular Docking Simulation; D009389:Neovascularization, Pathologic / Q000188:drug therapy / Q000473:pathology; D013329:Structure-Activity Relationship; D013629:Tamoxifen / Q000494:pharmacology; D042461:Vascular Endothelial Growth Factor A / Q000037:antagonists & inhibitors
D020533:Angiogenesis Inhibitors; D001562:Benzimidazoles; D042461:Vascular Endothelial Growth Factor A; D013629:Tamoxifen
2-(2-Furyl)-1H-benzimidazoles; Angiogenesis; Cytotoxicity; Molecular modeling; Vascular endothelial growth factor (VEGF)