39959-98-3Relevant academic research and scientific papers
Pyrazolopyrimidine derivatives as PI3 kinase inhibitors
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, (2015/09/22)
PI3Kβ selective compounds having the structure
3a,4-Dihydropyrazolo[1,5 a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase β Inhibitors
Yu, Hongyi,Moore, Michael L.,Erhard, Karl,Hardwicke, Mary Ann,Lin, Hong,Luengo, Juan I.,McSurdy-Freed, Jeanelle,Plant, Ramona,Qu, Junya,Raha, Kaushik,Rominger, Cynthia M.,Schaber, Michael D.,Spengler, Michael D.,Rivero, Ralph A.
, p. 230 - 234 (2013/03/28)
A series of novel [3a,4]dihydropyrazolo[1,5a]pyrimidines were identified, which were highly potent and selective inhibitors of PI3Kβ. The template afforded the opportunity to develop novel SAR for both the hinge-binding (R 3) and back-pocket (R4) substitutents. While cellular potency was relatively modest due to high protein binding, the series displayed low clearance in rat, mouse, and monkey.
