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Novel pyrazolo[1,5-a]pyridines with improved aqueous solubility as p110α-selective PI3 kinase inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2017 Jan 15; Vol. 27 (2), pp. 187-190. Date of Electronic Publication: 2016 Nov 25. - Publication Year :
- 2017
-
Abstract
- As part of our investigation into pyrazolo[1,5-a]pyridines as novel p110α selective PI3 kinase inhibitors, we report a range of analogues with improved aqueous solubility by the addition of a basic amine. The compounds demonstrated comparable p110α potency and selectivity to earlier compounds but with up to 1000× greater aqueous solubility, as the hydrochloride salts. The compounds also displayed good activity in a cellular assay of PI3 kinase activity.<br /> (Copyright © 2016 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Cell Line, Tumor
Cell Proliferation drug effects
Humans
Hydrazones chemical synthesis
Hydrazones pharmacology
Hydrazones toxicity
Mice
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors toxicity
Pyrazoles chemical synthesis
Pyrazoles toxicity
Pyridines chemical synthesis
Pyridines toxicity
Solubility
Phosphoinositide-3 Kinase Inhibitors
Protein Kinase Inhibitors pharmacology
Pyrazoles pharmacology
Pyridines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 27
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 27923617
- Full Text :
- https://doi.org/10.1016/j.bmcl.2016.11.078