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Imidazo[1,2- b ]pyridazines: a potent and selective class of cyclin-dependent kinase inhibitors
- Source :
- Bioorganic & Medicinal Chemistry Letters. 14:2249-2252
- Publication Year :
- 2004
- Publisher :
- Elsevier BV, 2004.
-
Abstract
- Modification of imidazo[1,2-a]pyridine CDK inhibitors lead to identification of less lipophilic imidazo[1,2-b]pyridazine series of CDK inhibitors. Although several equivalent compounds from these two series have similar structure and show similar CDK activity, the SAR of the two series differs significantly. Protein inhibitor structure determination has confirmed differences in binding mode and given some understanding of these differences in SAR. Potent and selective imidazo[1,2-b]pyridazine inhibitors of CDK2 have been identified, which show >1 microM plasma levels following a 2mg/kg oral dose to mice.
- Subjects :
- Models, Molecular
Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Biochemistry
Chemical synthesis
Pyridazine
Mice
chemistry.chemical_compound
Cyclin-dependent kinase
Drug Discovery
Animals
Enzyme Inhibitors
Protein kinase A
Molecular Biology
chemistry.chemical_classification
biology
Bicyclic molecule
Chemistry
Organic Chemistry
Cyclin-dependent kinase 2
Cyclin-Dependent Kinases
Pyridazines
Enzyme
Enzyme inhibitor
biology.protein
Molecular Medicine
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 14
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....0ae716885fecc6cff679ebaef4ca6a51