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.
Imbach
P
P
Novartis Pharmaceuticals, Novartis Limited, Basel, Switzerland.
Capraro
H G
HG
Furet
P
P
Mett
H
H
Meyer
T
T
Zimmermann
J
J
D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D016203:CDC2 Protein Kinase / Q000037:antagonists & inhibitors*; D017868:Cyclic AMP-Dependent Protein Kinases / Q000037:antagonists & inhibitors; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D004815:Epidermal Growth Factor / Q000037:antagonists & inhibitors; D006801:Humans; D007527:Isoenzymes / Q000037:antagonists & inhibitors; D007701:Kinetin; D011493:Protein Kinase C / Q000037:antagonists & inhibitors; D051571:Protein Kinase C-alpha; D011687:Purines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship