Synthesis of C2 alkynylated purines, a new family of potent inhibitors of cyclin-dependent kinases

M Legraverend; O Ludwig; E Bisagni; S Leclerc; L Meijer

doi:10.1016/s0960-894x(98)00097-3

Synthesis of C2 alkynylated purines, a new family of potent inhibitors of cyclin-dependent kinases

Bioorg Med Chem Lett. 1998 Apr 7;8(7):793-8. doi: 10.1016/s0960-894x(98)00097-3.

Authors

M Legraverend¹, O Ludwig, E Bisagni, S Leclerc, L Meijer

Affiliation

¹ UMR 176 CNRS, Institut Curie, Section de Recherche, Centre Universitaire, Orsay, France. Michel.Legraverend@curie.u-psud.fr

PMID: 9871543
DOI: 10.1016/s0960-894x(98)00097-3

Abstract

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.

MeSH terms

Alkynes / chemical synthesis*
Alkynes / chemistry
Alkynes / pharmacology
Animals
CDC2 Protein Kinase / antagonists & inhibitors*
CDC2 Protein Kinase / isolation & purification
Cyclin B / antagonists & inhibitors
Cyclin-Dependent Kinases / antagonists & inhibitors*
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology
Female
Kinetin
Oocytes / enzymology
Purines / chemical synthesis*
Purines / chemistry
Purines / pharmacology
Roscovitine
Starfish
Structure-Activity Relationship

Substances

Alkynes
Cyclin B
Enzyme Inhibitors
Purines
Roscovitine
olomoucine
CDC2 Protein Kinase
Cyclin-Dependent Kinases
Kinetin