1137278-42-2Relevant articles and documents
Potent and highly selective benzimidazole inhibitors of PI3-kinase delta
Murray, Jeremy M.,Sweeney, Zachary K.,Chan, Bryan K.,Balazs, Mercedesz,Bradley, Erin,Castanedo, Georgette,Chabot, Christine,Chantry, David,Flagella, Michael,Goldstein, David M.,Kondru, Rama,Lesnick, John,Li, Jun,Lucas, Matthew C.,Nonomiya, Jim,Pang, Jodie,Price, Stephen,Salphati, Laurent,Safina, Brian,Savy, Pascal P. A.,Seward, Eileen M.,Ultsch, Mark,Sutherlin, Daniel P.
, p. 7686 - 7695 (2012/10/29)
Inhibition of PI3Kδ is considered to be an attractive mechanism for the treatment of inflammatory diseases and leukocyte malignancies. Using a structure-based design approach, we have identified a series of potent and selective benzimidazole-based inhibitors of PI3Kδ. These inhibitors do not occupy the selectivity pocket between Trp760 and Met752 that is induced by other families of PI3Kδ inhibitors. Instead, the selectivity of the compounds for inhibition of PI3Kδ relative to other PI3K isoforms appears to be due primarily to the strong interactions these inhibitors are able to make with Trp760 in the PI3Kδ binding pocket. The pharmacokinetic properties and the ability of compound 5 to inhibit the function of B-cells in vivo are described.
THIAZOLOPYRIMIDINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE
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Page/Page column 93, (2009/05/29)
Compounds of Formulas (Ia and Ib), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed
