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Triazolo[1,5-a]pyrimidines as novel CDK2 inhibitors: protein structure-guided design and SAR.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Mar 01; Vol. 16 (5), pp. 1353-7. Date of Electronic Publication: 2005 Dec 01. - Publication Year :
- 2006
-
Abstract
- Crystallographic and modelling data, in conjunction with a medicinal chemistry template-hopping approach, led to the identification of a series of novel and potent inhibitors of human cyclin-dependent kinase 2 (CDK2), with selectivity over glycogen synthase kinase-3beta (GSK-3beta). One example had a CDK2 IC(50) of 120 nM and showed selectivity over GSK-3beta of 167-fold.
- Subjects :
- Cell Line, Tumor
Cyclin-Dependent Kinase 2 metabolism
Humans
Inhibitory Concentration 50
Molecular Structure
Protein Kinase Inhibitors chemistry
Pyrimidines chemical synthesis
Structure-Activity Relationship
Cyclin-Dependent Kinase 2 antagonists & inhibitors
Drug Design
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors pharmacology
Pyrimidines chemistry
Pyrimidines pharmacology
Triazoles chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 16
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 16325401
- Full Text :
- https://doi.org/10.1016/j.bmcl.2005.11.048