Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1362520 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
PI3 Kinases are a family of lipid kinases mediating numerous cell processes such as proliferation, migration, and differentiation. The PI3 kinase pathway is often de-regulated in cancer through PI3Kα overexpression, gene amplification, mutations, and PTEN phosphatase deletion. PI3K inhibitors represent therefore an attractive therapeutic modality for cancer treatment. Herein we describe a novel series of PI3K inhibitors sharing a pyrimidine core and showing significant potency against class I PI3 kinases in the biochemical assay and in cells. The discovery, synthesis and SAR of this chemotype are described.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Sabina Pecchi, Paul A. Renhowe, Clarke Taylor, Susan Kaufman, Hanne Merritt, Marion Wiesmann, Kevin R. Shoemaker, Mark S. Knapp, Elizabeth Ornelas, Thomas F. Hendrickson, Wendy Fantl, Charles F. Voliva,