Imbach-Weese, Patricia, Gerspacher, Marc, Caravatti, Giorgio, Furet, Pascal, Zoller, Thomas, Fritsch, Christine, Haasen, Dorothea, Trappe, Joerg, Guthy, Daniel Alexander, Arz, Dorothee and Wirth, Jasmin (2015) Identification and optimisation of a 4',5-bisthiazole series of selective phosphatidylinositol-3 kinase alpha inhibitors. Bioorganic and Medicinal Chemistry Letters, 25. pp. 3569-3574.

Abstract

Abstract: Exploring the affinity-pocket binding moiety of a 2-aminothiazole (S)-proline-amide-urea series of selective PI3Kα inhibitors using a parallel-synthesis approach led to the identification of a novel 4',5-bisthiazole sub-series. The synthesis and optimisation of both the affinity pocket and (S)-proline amide moieties within this 4',5-bisthiazole sub-series are described. From this work a number of analogues, including 14 (A66) and 24, were identified as potent and selective PI3Kα inhibitor in vitro tool compounds.

Item Type:	Article
Keywords:	Oncology, kinase inhibitor, phosphatidylinositol-3-kinase-alpha
Date Deposited:	03 Nov 2015 00:45
Last Modified:	03 Nov 2015 00:45
URI:	https://oak.novartis.com/id/eprint/25253