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Kinase inhibitions in pyrido[4,3-h] and [3,4-g]quinazolines: Synthesis, SAR and molecular modeling studies.
- Source :
-
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2019 May 15; Vol. 27 (10), pp. 2083-2089. Date of Electronic Publication: 2019 Apr 04. - Publication Year :
- 2019
-
Abstract
- New pyrido[3,4-g]quinazoline derivatives were prepared and evaluated for their inhibitory potency toward 5 protein kinases (CLK1, DYRK1A, GSK3, CDK5, CK1). A related pyrido[4,3-h]quinazoline scaffold with an angular structure was also synthesized and its potency against the same protein kinase panel was compared to the analogous pyrido[3,4-g]quinazoline. Best results were obtained for 10-nitropyrido[3,4-g]quinazoline 4 toward CLK1 with nanomolar activities.<br /> (Copyright © 2019 Elsevier Ltd. All rights reserved.)
- Subjects :
- Cyclin-Dependent Kinase 5 antagonists & inhibitors
Cyclin-Dependent Kinase 5 metabolism
Glycogen Synthase Kinase 3 antagonists & inhibitors
Glycogen Synthase Kinase 3 metabolism
Humans
Molecular Docking Simulation
Protein Kinase Inhibitors metabolism
Protein Kinases chemistry
Protein Serine-Threonine Kinases antagonists & inhibitors
Protein Serine-Threonine Kinases metabolism
Protein Structure, Tertiary
Protein-Tyrosine Kinases antagonists & inhibitors
Protein-Tyrosine Kinases metabolism
Quinazolines metabolism
Structure-Activity Relationship
Protein Kinase Inhibitors chemical synthesis
Protein Kinases metabolism
Pyridines chemistry
Quinazolines chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3391
- Volume :
- 27
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 30967303
- Full Text :
- https://doi.org/10.1016/j.bmc.2019.04.005