2,6,9-trisubstituted purines : Optimization towards highly potent and selective CDK1 inhibitors

Novel 2,6,9-substituted purine derivatives represent a class of potent and selective inhibitors of CDK1/cyclinB. The synthesis, SAR and biological profile of selected compounds are described. Novel 2,6,9-substituted purine derivatives represent a class of potent and selective inhibitors of CDK1/cycl...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1999-01, Vol.9 (1), p.91-96
Main Authors: Imbach, Patricia, Capraro, Hans-Georg, Furet, Pascal, Mett, Helmut, Meyer, Thomas, Zimmermann, Jürg
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biological and medical sciences
CDC2 Protein Kinase - antagonists & inhibitors
Cyclic AMP-Dependent Protein Kinases - antagonists & inhibitors
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Epidermal Growth Factor - antagonists & inhibitors
General aspects
Humans
Isoenzymes - antagonists & inhibitors
Kinetin
Medical sciences
Pharmacology. Drug treatments
Protein Kinase C - antagonists & inhibitors
Protein Kinase C-alpha
Purines - chemical synthesis
Purines - chemistry
Purines - pharmacology
Structure-Activity Relationship
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Summary:Novel 2,6,9-substituted purine derivatives represent a class of potent and selective inhibitors of CDK1/cyclinB. The synthesis, SAR and biological profile of selected compounds are described. Novel 2,6,9-substituted purine derivatives represent a class of potent and selective inhibitors of CDK1/cyclinB. The synthesis, SAR and biological profile of selected compounds are described.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(98)00691-X