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

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

  • Bioorg Med Chem Lett. 2009 Jun 15;19(12):3166-9. doi: 10.1016/j.bmcl.2009.04.122.
Masaharu Uno 1,  Hyun Seung Ban,  Hiroyuki Nakamura
Affiliations

Affiliation

  • 1 Department of Chemistry, Faculty of Science, Gakushuin University, Mejiro, Tokyo 171-8588, Japan.
PMID: 19435661 DOI: 10.1016/j.bmcl.2009.04.122
Abstract

A series of 1-[4-(N-benzylamino)phenyl]-3-phenylurea derivatives 2a-r were synthesized as HIF-1alpha inhibitors. Among the compounds synthesized, compound 2k was found to be a potent inhibitor against HIF-1alpha accumulation under hypoxic condition and inhibited the hypoxia-induced HIF-1 transcriptional activity in HEK293 cells (IC(50)=7.2 microM). Furthermore, compound 2k suppressed the hypoxia-induced secretion of VEGF in HeLa cells (IC(50)=15 microM).

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