Title : Synthesis, in vitro anticancer activity and in silico studies of certain isoxazole-based carboxamides, ureates, and hydrazones as potential inhibitors of VEGFR2.

Pub. Date : 2021 Nov

PMID : 34534755






3 Functional Relationships(s)
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1 Evaluation of growth inhibitory activity of the synthesized compounds against hepatocellular carcinoma (HepG2), that overexpresses VEGFR2, showed superior activity of compounds 8, 10a and 10c with IC50 in sub micromolar concentrations of 0.84, 0.79 and 0.69 muM, respectively, which is better than that of the reference drug, Sorafenib (IC50 = 3.99 microM). Sorafenib kinase insert domain receptor Homo sapiens
2 The results of VEGFR2 kinase inhibition assay demonstrate that, compounds 8 and 10a are the most active inhibitors with IC50 = 25.7 and 28.2 nM, respectively, (Sorafenib IC50 = 28.1 nM). Sorafenib kinase insert domain receptor Homo sapiens
3 Molecular docking of the synthesized derivatives to VEGFR2 (PDB: 3WZE) showed similar binding modes to that of the co-crystallized ligand, sorafenib. Sorafenib kinase insert domain receptor Homo sapiens