Synthesis of C2 alkynylated purines, a new family of potent inhibitors of cyclin-dependent kinases.
The synthesis of a new family of inhibitors of the cell cycle regulating cyclin-dependent kinases (CDK's) is reported. These compounds, related to the purines olomoucine and roscovitine, are characterised by the presence of alkynylated side chains at C2. They inhibit CDK's with IC50's in the 200 nM range.
Legraverend
M
M
UMR 176 CNRS, Institut Curie, Section de Recherche, Centre Universitaire, Orsay, France. Michel.Legraverend@curie.u-psud.fr
Ludwig
O
O
Bisagni
E
E
Leclerc
S
S
Meijer
L
L
D000480:Alkynes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D016203:CDC2 Protein Kinase / Q000037:antagonists & inhibitors* / Q000302:isolation & purification; D019926:Cyclin B / Q000037:antagonists & inhibitors; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005260:Female; D007701:Kinetin; D009865:Oocytes / Q000201:enzymology; D011687:Purines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000077546:Roscovitine; D013215:Starfish; D013329:Structure-Activity Relationship
D000480:Alkynes; D019926:Cyclin B; D004791:Enzyme Inhibitors; D011687:Purines; D000077546:Roscovitine; C090046:olomoucine; D016203:CDC2 Protein Kinase; D018844:Cyclin-Dependent Kinases; D007701:Kinetin