1374306-11-2Relevant articles and documents
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
Sanchez, Robert M.,Erhard, Karl,Hardwicke, Mary Ann,Lin, Hong,McSurdy-Freed, Jeanelle,Plant, Ramona,Raha, Kaushik,Rominger, Cynthia M.,Schaber, Michael D.,Spengler, Michael D.,Moore, Michael L.,Yu, Hongyi,Luengo, Juan I.,Tedesco, Rosanna,Rivero, Ralph A.
, p. 3198 - 3202 (2012/06/29)
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 IC50) growth inhibition in a PTEN deficient cancer cell line.