Design, synthesis and preliminary biological evaluation of purine-2,6-diamine derivatives as cyclin-dependent kinase (CDK) inhibitors

Article abstract of DOI:10.1002/cjoc.201300420

Novel purine-2,6-diamine derivatives were designed and synthesized as cyclin-dependent kinase (CDK) inhibitors. According to the preliminary biological evaluation, most of the compounds show good inhibitory activities in CDK1 enzyme assay and potent antiproliferative activities in some tumor cell lines. Especially, compound 11a (IC₅₀=0.35 μmol/L for CDK1/cyclin B and IC₅₀=0.023 μmol/L for CDK2/cyclin A) possessed better inhibitory effect compared with Roscovitine (IC₅₀=2.54 (mol/L for CDK1/cyclin B and IC₅₀=0.092 μmol/L for CDK2/cyclin A). Copyright