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Benzodipyrazoles: a new class of potent CDK2 inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2005 Mar 01; Vol. 15 (5), pp. 1315-9. - Publication Year :
- 2005
-
Abstract
- The synthesis and the preliminary expansion of this new class of CDK2 inhibitors are presented. The synthesis was accomplished using a solution-phase protocol amenable to rapid parallel expansion and suitable to be scaled-up in view of possible lead development. Following a medicinal chemistry program aimed at improving cell permeability and selectivity, a series of compounds with nanomolar activity in the biochemical assay and able to efficiently inhibit tumor cell proliferation has been obtained.
- Subjects :
- Cell Line, Tumor
Cell Proliferation drug effects
Crystallization
Crystallography, X-Ray
Cyclin A antagonists & inhibitors
Cyclin-Dependent Kinase 2
Enzyme Inhibitors chemical synthesis
Glycogen Synthase Kinase 3 antagonists & inhibitors
Humans
Models, Molecular
Molecular Structure
Pyrazoles chemical synthesis
Structure-Activity Relationship
CDC2-CDC28 Kinases antagonists & inhibitors
Enzyme Inhibitors classification
Enzyme Inhibitors pharmacology
Pyrazoles classification
Pyrazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 15
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 15713378
- Full Text :
- https://doi.org/10.1016/j.bmcl.2005.01.023