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

P Imbach; H G Capraro; P Furet; H Mett; T Meyer; J Zimmermann

doi:10.1016/s0960-894x(98)00691-x

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

Bioorg Med Chem Lett. 1999 Jan 4;9(1):91-6. doi: 10.1016/s0960-894x(98)00691-x.

Authors

P Imbach¹, H G Capraro, P Furet, H Mett, T Meyer, J Zimmermann

Affiliation

¹ Novartis Pharmaceuticals, Novartis Limited, Basel, Switzerland.

PMID: 9990463
DOI: 10.1016/s0960-894x(98)00691-x

Abstract

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.

MeSH terms

Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology
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
Humans
Isoenzymes / antagonists & inhibitors
Kinetin
Protein Kinase C / antagonists & inhibitors
Protein Kinase C-alpha
Purines / chemical synthesis
Purines / chemistry*
Purines / pharmacology*
Structure-Activity Relationship

Substances

Antineoplastic Agents
Enzyme Inhibitors
Isoenzymes
Purines
Epidermal Growth Factor
olomoucine
Cyclic AMP-Dependent Protein Kinases
PRKCA protein, human
Protein Kinase C
Protein Kinase C-alpha
CDC2 Protein Kinase
Kinetin