期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 9, 页码 3198-3202出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.03.039
关键词
PI3K-beta inhibitor; PTEN-deficient; Phosphatidylinositol 3-kinase; Triazolopyrimidinone; Structure-activity relationship
A series of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones with excellent enzyme inhibition, improved isoform selectivity, and excellent inhibition of downstream phosphorylation of AKT has been identified. Several compounds in the series demonstrated potent (similar to 0.100 mu M IC50) growth inhibition in a PTEN deficient cancer cell line. (C) 2012 Elsevier Ltd. All rights reserved.
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