Identification and Structure-Activity Relationship of 2-Morpholino 6-(3-Hydroxyphenyl) Pyrimidines, a Class of Potent and Selective PI3-Kinase Inhibitors
Tools
Tools
Pecchi, Sabina, Renhowe, Paul, Taylor, Clarke, Kaufman, Susan, Merritt, Hanne, Wiesmann, Marion, Shoemaker, Kevin, Knapp, Mark, Hendrickson, Thomas, Fantl, Wendy and Voliva, Charles (2011) Identification and Structure-Activity Relationship of 2-Morpholino 6-(3-Hydroxyphenyl) Pyrimidines, a Class of Potent and Selective PI3-Kinase Inhibitors. Bioorganic and Medicinal Chemistry Letters, 20 (23). pp. 6895-6898. ISSN 0960-894X
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 PI3K alpha 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 IA PI3 kinases in the biochemical assay and in cells. The discovery, synthesis and SAR of this chemotype are described.
| Item Type: | Article |
|---|---|
| Related URLs: | |
| Related URLs: | |
| Date Deposited: | 13 Oct 2015 13:16 |
| Last Modified: | 13 Oct 2015 13:16 |
| URI: | https://oak.novartis.com/id/eprint/3162 |