| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1370863 | Bioorganic & Medicinal Chemistry Letters | 2015 | 7 Pages |
Abstract
In this report we detail the evolution of our previously reported thiophene isoxazole BET inhibitor chemotype exemplified by CPI-3 to a novel bromodomain selective chemotype (the methyl isoxazoleazepine chemotype) exemplified by carboxamide 23. The methyl isoxazoleazepine chemotype provides potent inhibition of the bromodomains of the BET family, excellent in vivo PK across species, low unbound clearance, and target engagement in a MYC PK-PD model.
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Related Topics
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Organic Chemistry
Authors
Michael C. Hewitt, Yves Leblanc, Victor S. Gehling, Rishi G. Vaswani, Alexandre Côté, Christopher G. Nasveschuk, Alexander M. Taylor, Jean-Christophe Harmange, James E. Audia, Eneida Pardo, Rich Cummings, Shivangi Joshi, Peter Sandy, Jennifer A. Mertz,