Author/Authors :
Roberto D’Alessio، نويسنده , , Alberto Bargiotti، نويسنده , , Suzanne Metz، نويسنده , , M. Gabriella Brasca، نويسنده , , Alexander Cameron، نويسنده , , Antonella Ermoli، نويسنده , , Aurelio Marsiglio، نويسنده , , Paolo Polucci، نويسنده , , Fulvia Roletto، نويسنده , , Marcellino Tibolla، نويسنده , , Michael L. Vazquez، نويسنده , , Anna Vulpetti، نويسنده , , Paolo Pevarello، نويسنده ,
Abstract :
The synthesis and the preliminary expansion of this new class of CDK2 inhibitors are presented. The synthesis was accomplished using a solution-phase protocol amenable to rapid parallel expansion and suitable to be scaled-up in view of possible lead development. Following a medicinal chemistry program aimed at improving cell permeability and selectivity, a series of compounds with nanomolar activity in the biochemical assay and able to efficiently inhibit tumor cell proliferation has been obtained.
Keywords :
Tumor cell proliferation inhibition , CDK2 , Kinase selectivity , cyclins
