Fragment based discovery of arginine isosteres through REPLACE: Towards non-ATP competitive CDK inhibitors
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چکیده
منابع مشابه
Triazole-linked reduced amide isosteres: an approach for the fragment-based drug discovery of anti-Alzheimer's BACE1 inhibitors.
In the course of a β-site APP-cleaving enzyme 1 (BACE1) inhibitor discovery project an in situ synthesis/screening protocol was employed to prepare 120 triazole-linked reduced amide isostere inhibitors. Among these compounds, four showed modest (single digit micromolar) BACE1 inhibition. Our ligand design was based on a potent reduced amide isostere 1, wherein the P(2) amide moiety was replaced...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry
سال: 2014
ISSN: 0968-0896
DOI: 10.1016/j.bmc.2013.10.039