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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. | LitMetric
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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

Bioorg Med Chem Lett

Cancer Metabolism Chemistry, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA.

Published: May 2012

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 (∼ 0.100 μM IC(50)) growth inhibition in a PTEN deficient cancer cell line.

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 Source
http://dx.doi.org/10.1016/j.bmcl.2012.03.039DOI Listing

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