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ID: ALA1153990

Journal: Bioorg Med Chem Lett

Title: Exploring the PI3K alpha and gamma binding sites with 2,6-disubstituted isonicotinic derivatives.

Authors: Cherian PT, Koikov LN, Wortman MD, Knittel JJ.

Abstract: A homology model of the p110alpha catalytic subunit of PI3Kalpha was generated from the p110gamma crystal structure. Using this model, an isonicotinic scaffold was designed for chemically exploring the PI3Kalpha and gamma binding sites. A focused library of derivatives was synthesized and tested. The morpholine acids 5a and 5b proved to be the most potent analogs.

CiteXplore: 19297156

DOI: 10.1016/j.bmcl.2009.02.115