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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 PI3Kα inhibitor with high PI3K isoform selectivity and potent cellular activity.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015 Sep 01; Vol. 25 (17), pp. 3582-4. Date of Electronic Publication: 2015 Jun 30. - Publication Year :
- 2015
-
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 PI3Kα inhibitor with favorable physicochemical and PK-properties is described.<br /> (Copyright © 2015 Elsevier Ltd. All rights reserved.)
- Subjects :
- Amination
Animals
Class I Phosphatidylinositol 3-Kinases
Humans
Models, Molecular
Neoplasms drug therapy
Neoplasms enzymology
Phosphatidylinositol 3-Kinases chemistry
Phosphatidylinositol 3-Kinases metabolism
Protein Kinase Inhibitors pharmacokinetics
Pyridines pharmacokinetics
Rats
Thiazoles pharmacokinetics
Phosphoinositide-3 Kinase Inhibitors
Protein Kinase Inhibitors chemistry
Protein Kinase Inhibitors pharmacology
Pyridines chemistry
Pyridines pharmacology
Thiazoles chemistry
Thiazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 25
- Issue :
- 17
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 26164189
- Full Text :
- https://doi.org/10.1016/j.bmcl.2015.06.077