Yuan, Xu published the artcileDesign, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase, Computed Properties of 104-01-8, the main research area is amide aryl benzoxazole preparation antitumor antiangiogenesis VEGFR2 tyrosine kinase; benzimidazole amide aryl preparation antitumor antiangiogenesis VEGFR2 tyrosine kinase; Angiogenesis; Antitumor activity; Benzimidazole; Benzoxazole; VEGFR-2.
A library of thirty-seven 6-amide-2-aryl benzoxazoles I (R1 = H, F, Br, Cl and MeO; R2 = F, Br, Cl, Me and MeO; R3 = H and MeO; X = O; X1 = H and Cl; X2 = H, 2-F, 2-Cl, 2-Br and 3-Br; n = 0, 1)/benzimidazoles I (R1 = H, F, Br and MeO; R2 = Cl, Me and MeO; R3 = H and MeO; R3 = Cl, Me and OMe; X = NH; X1 = Cl; X2 = H; n = 0, 1) has been designed and synthesized based on the highly conserved active site of VEGFR-2. Several title compounds I exhibited selective inhibitory activities against VEGFR-2 than EGFR kinases, which also displayed selective anti-proliferation potency against the HUVEC and HepG2 than the A549 and MDA-MB-231 cancer cell lines. The newly synthesized compounds I were evaluated for anti-angiogenesis capability by chick chorioallantoic membrane (CAM) assay. Among them, compounds I (R1 = R3 = H; R2 = OMe; n = 1; X = NH; X1 = Cl; X2 = H) showed the most potent anti-angiogenesis ability (79% inhibition at 10 nM/eggs), the efficient cytotoxic activities (in vitro against the HUVEC and HepG2 cell lines with IC50 values of 1.47 and 2.57 μM, resp.), and excellent VEGFR-2 kinase inhibition (IC50 = 0.051 μM). The mol. docking anal. revealed that compound I (R1 = R3 = H; R2 = OMe; n = 1; X = NH; X1 = Cl; X2 = H) is a Type II inhibitor of VEGFR-2 kinase. These results indicated that the 6-amide-2-arylbenzoxazoles and 6-amide-2-aryl benzimidazoles I are promising inhibitors of VEGFR-2 kinase for the potential treatment of anti-angiogenesis.
European Journal of Medicinal Chemistry published new progress about Angiogenesis. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Computed Properties of 104-01-8.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem