1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1 alpha inhibitors

[摘要]：A series of 1-[4-(N-benzylamino)phenyl]-3-phenylurea derivatives 2a-r were synthesized as HIF-1 alpha inhibitors. Among the compounds synthesized, compound 2k was found to be a potent inhibitor against HIF-1 alpha accumulation under hypoxic condition and inhibited the hypoxia-induced HIF-1 transcriptional activity in HEK293 cells (IC50 = 7.2 mu M). Furthermore, compound 2k suppressed the hypoxia-induced secretion of VEGF in HeLa cells (IC50 = 15 mu M). (C) 2009 Elsevier Ltd. All rights reserved.

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