Design, synthesis, molecular docking and cytotoxic evaluation of novel 2-furybenzimidazoles as VEGFR-2 inhibitors

European Journal of Medicinal Chemistry
Mona A AbdullazizHoda I El Diwani

Abstract

Inhibition of angiogenesis through inhibition of vascular endothelial growth factor receptor 2 (VEGFR-2) has been applied in cancer therapy because of its important role in promoting cancer growth and metastasis. In the presented study, a series of benzimidazol-furan hybrids was designed and synthesized through facile synthetic pathways. Evaluation of the synthesized compounds for their in vitro cytotoxic activity against breast (MCF-7) and hepatocellular (HepG2) carcinoma cell lines was performed. Two of the synthesized conjugates, 10b and 15, showed potent antiproliferative properties against MCF-7 cell line (IC50 = 21.25, 21.35 μM, respectively) in comparison to tamoxifen (IC50 = 21.57 μM). Additionally, compounds 10a, 10b, 15 and 17 showed promising potency (IC50 = 25.95, 22.58, 26.94 and 31.06 μM, respectively) against liver carcinoma cell line HepG2 in contrast to cisplatin (IC50 = 31.16 μM). Moreover, in vitro evaluation of the synthesized compounds for their effect on the level of VEGFR-2 in MCF-7 cell line showed their potent inhibitory activity relative to control untreated cells. Four compounds 10a, 10b, 14 and 15 showed 92-96% reduction in VEGFR-2 level, compared with tamoxifen and sorafenib which showed inhibition ...Continue Reading

Citations

Feb 15, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Heba T Abdel-MohsenMathias O Senge
Sep 23, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Abd El-Galil E AmrElsayed A Elsayed
Dec 6, 2017·Archiv der Pharmazie·Parameshwar RavulaJanivara Nanjunde Gowda Narendra Sharath Chandra
Nov 21, 2020·Bioorganic & Medicinal Chemistry·Khaled El-AdlIbrahim H Eissa

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