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Co-immunoprecipitation Assay Using Endogenous Nuclear Proteins from Cells Cultured Under Hypoxic Conditions
Published on: August 2, 2018
Synthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1α inhibitors
Wenwei Huang1, Ruili Huang, Matias S Attene-Ramos
1NIH 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.
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