Literature DB >> 19435661

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

Masaharu Uno1, Hyun Seung Ban, Hiroyuki Nakamura.   

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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Year:  2009        PMID: 19435661     DOI: 10.1016/j.bmcl.2009.04.122

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1α inhibitors.

Authors:  Wenwei Huang; Ruili Huang; Matias S Attene-Ramos; Srilatha Sakamuru; Erika E Englund; James Inglese; Christopher P Austin; Menghang Xia
Journal:  Bioorg Med Chem Lett       Date:  2011-07-21       Impact factor: 2.823

2.  Discovery of Indenopyrazoles as a New Class of Hypoxia Inducible Factor (HIF)-1 Inhibitors.

Authors:  Hidemitsu Minegishi; Shinji Fukashiro; Hyun Seung Ban; Hiroyuki Nakamura
Journal:  ACS Med Chem Lett       Date:  2013-01-27       Impact factor: 4.345

3.  Highly Regioselective Synthesis of Substituted Isoindolinones via Ruthenium-Catalyzed Alkyne Cyclotrimerizations.

Authors:  Robert W Foster; Christopher J Tame; Helen C Hailes; Tom D Sheppard
Journal:  Adv Synth Catal       Date:  2013-08-12       Impact factor: 5.837

  3 in total

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