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

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

  • Bioorg Med Chem Lett. 2011 Sep 15;21(18):5239-43. doi: 10.1016/j.bmcl.2011.07.043.
Wenwei Huang 1,  Ruili Huang,  Matias S Attene-Ramos,  Srilatha Sakamuru,  Erika E Englund,  James Inglese,  Christopher P Austin,  Menghang Xia
Affiliations

Affiliation

  • 1 NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Dr., Rockville, MD 20850, USA. huangwe@mail.nih.gov
PMID: 21831635 DOI: 10.1016/j.bmcl.2011.07.043
Abstract

Quinazolin-4-one 1 was identified as an inhibitor of the HIF-1α transcriptional factor from a high-throughput screen. HIF-1α up-regulation is common in many Cancer cells. In this Letter, we describe an efficient one-pot sequential reaction for the synthesis of quinazolin-4-one 1 analogues. The structure-activity relationship (SAR) study led to the 5-fold more potent analogue, 16.

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