Imbach-Weese, Patricia and Gerspacher, Marc and Caravatti, Giorgio and Furet, Pascal and Zoller, Thomas and Fritsch, Christine and Haasen, Dorothea and Trappe, Joerg and Guthy, Daniel Alexander and 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