Synthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potent β isoform selective phosphatidylinositol 3-kinase inhibitors.

Robert M Sanchez,Karl Erhard,Mary Ann Hardwicke,Hong Lin,Jeanelle McSurdy-Freed,Ramona Plant,Kaushik Raha,Cynthia M Rominger,Michael D Schaber,Michael D Spengler,Michael L Moore,Hongyi Yu,Juan I Luengo,Rosanna Tedesco,Ralph A Rivero

Bioorganic & Medicinal Chemistry Letters（2012）

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摘要

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 (∼ 0.100μM IC50) growth inhibition in a PTEN deficient cancer cell line.

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关键词

PI3K-β inhibitor,PTEN-deficient,Phosphatidylinositol 3-kinase,Triazolopyrimidinone,Structure–activity relationship

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