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ID: ALA1140511
Journal: Bioorg Med Chem Lett
Title: Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1alpha inhibitors.
Authors: Boovanahalli SK, Jin X, Jin Y, Kim JH, Dat NT, Hong YS, Lee JH, Jung SH, Lee K, Lee JJ.
Abstract: We report a new series of HIF-1alpha inhibitors which were obtained through structural modifications of previously reported lead 1. The in vitro inhibitory potencies of newly synthesized compounds were evaluated against hypoxia-induced HIF-1 activation using cell-based reporter assay in three human cancer cell lines including SK-Hep-1, Hep3B, and AGS cells. Several compounds displayed significant inhibitory activity in all the three tested cell lines. In particular, analogue 17 displayed potent inhibition of hypoxia-induced accumulation of HIF-1alpha protein in Hep3B cell line, in addition to the dose-dependent inhibition of HIF-1 target genes VEGF and EPO.
CiteXplore: 17884495