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Bioorg Med Chem Lett. 2011 Sep 15;21(18):5239-43. doi: 10.1016/j.bmcl.2011.07.043. Epub 2011 Jul 21.

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

Author information

1
NIH Chemical Genomics Center, National Human Genome Research Institute, NIH, 9800 Medical Center Dr., Rockville, MD 20850, USA. huangwe@mail.nih.gov

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.

PMID:
21831635
PMCID:
PMC3681418
DOI:
10.1016/j.bmcl.2011.07.043
[Indexed for MEDLINE]
Free PMC Article

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