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Discovery of a Novel Tricyclic 4H-Thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino Scaffold and its Application in a PI3K Inhibitor with High PI3K Isoform Selectivity and Potent Cellular Activity

Gerspacher, Marc and Fairhurst, Robin and Mah, Robert and Roehn-Carnemolla, Esther and Furet, Pascal and Fritsch, Christine and Guthy, Daniel Alexander (2015) Discovery of a Novel Tricyclic 4H-Thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino Scaffold and its Application in a PI3K Inhibitor with High PI3K Isoform Selectivity and Potent Cellular Activity. Bioorg. Med. Chem. Letters, 25 (17). pp. 3582-3584. ISSN 0960-894X

Abstract

A novel, previously undescribed 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine tricyclic scaffold has been discovered. The application of this novel chemotype leading to a potent and selective prototype PI3K inhibitor is described.

Item Type: Article
Keywords: Oncology, Phosphatidylinositol-3-kinase (PI3K), selective PI3K Inhibitor, 4H-Thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino derivative
Date Deposited: 12 Oct 2016 00:45
Last Modified: 12 Oct 2016 00:45
URI: https://oak.novartis.com/id/eprint/25268

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