Ontology highlight
ABSTRACT:
SUBMITTER: Yu H
PROVIDER: S-EPMC4027147 | biostudies-literature | 2013 Feb
REPOSITORIES: biostudies-literature
Yu Hongyi H Moore Michael L ML Erhard Karl K Hardwicke Mary Ann MA Lin Hong H Luengo Juan I JI McSurdy-Freed Jeanelle J Plant Ramona R Qu Junya J Raha Kaushik K Rominger Cynthia M CM Schaber Michael D MD Spengler Michael D MD Rivero Ralph A RA
ACS medicinal chemistry letters 20130110 2
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 (R3) 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. ...[more]