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Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors

Gerspacher, Marc and Imbach-Weese, Patricia and Mah, Robert and Caravatti, Giorgio and Furet, Pascal and Fritsch, Christine and Schnell, Christian and Blanz, Joachim and Blasco, Francesca and Desrayaud, Sandrine and Guthy, Daniel Alexander and Knapp, Mark and Arz, Dorothee and Wirth, Jasmin and Roehn-Carnemolla, Esther and Luu, Van Huy (2015) Identification and optimisation of 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole and 4,5-dihydrothiazolo[4,5-h]quinazoline series of selective phosphatidylinositol-3 kinase alpha inhibitors. Bioorganic and Medicinal Chemistry Letters, 25. pp. 3575-3581. ISSN 0960-894X

Abstract

Abstract: A cyclisation within a 4',5-bisthiazole (S)-proline-amide-urea series of selective PI3Kα inhibitors led to a novel 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole tricyclic sub-series. The synthesis and optimisation of this 4,5-dihydrobenzo[1,2-d:3,4-d]bisthiazole sub-series and the expansion to a related tricyclic 4,5-dihydrothiazolo[4,5-h]quinazoline sub-series are described. From this work analogues inclusing 11, 12, 19 and 23 were identified as potent and selective PI3Kα inhibitor in vivo tool compounds.

Item Type: Article
Keywords: Oncology, kinase inhibitor, phosphatidylinositol-3-kinase-alpha
Date Deposited: 13 Oct 2015 13:11
Last Modified: 13 Oct 2015 13:11
URI: https://oak.novartis.com/id/eprint/25254

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