Discovery of a novel tricyclic 4H-thiazolo[5',4':4,5]pyrano[2,3-c]pyridine-2-amino scaffold and its application in a PI3Kα inhibitor with high PI3K isoform selectivity and potent cellular activity.
Autor: | Gerspacher M; Novartis Institutes for BioMedical Research, Novartis Pharma AG, WKL-136.4.84, CH-4002 Basel, Switzerland. Electronic address: marc.gerspacher@novartis.com., Fairhurst RA; Novartis Institutes for BioMedical Research, Novartis Pharma AG, WKL-136.4.84, CH-4002 Basel, Switzerland., Mah R; Novartis Institutes for BioMedical Research, Novartis Pharma AG, WKL-136.4.84, CH-4002 Basel, Switzerland., Roehn-Carnemolla E; Novartis Institutes for BioMedical Research, Novartis Pharma AG, WKL-136.4.84, CH-4002 Basel, Switzerland., Furet P; Novartis Institutes for BioMedical Research, Novartis Pharma AG, WKL-136.4.84, CH-4002 Basel, Switzerland., Fritsch C; Novartis Institutes for BioMedical Research, Novartis Pharma AG, WKL-136.4.84, CH-4002 Basel, Switzerland., Guthy DA; Novartis Institutes for BioMedical Research, Novartis Pharma AG, WKL-136.4.84, CH-4002 Basel, Switzerland. |
---|---|
Jazyk: | angličtina |
Zdroj: | Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015 Sep 01; Vol. 25 (17), pp. 3582-4. Date of Electronic Publication: 2015 Jun 30. |
DOI: | 10.1016/j.bmcl.2015.06.077 |
Abstrakt: | 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 PI3Kα inhibitor with favorable physicochemical and PK-properties is described. (Copyright © 2015 Elsevier Ltd. All rights reserved.) |
Databáze: | MEDLINE |
Externí odkaz: |