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 (CDKʹs) is reported. These compounds, related to the purines olomoucine and roscovitine, are characterised by the presence of alkynylated side chains at C2. They inhibit CDKʹs with IC50ʹs in the 200 nM range.