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Keywords:

  • purine derivatives;
  • CDK inhibitors;
  • antitumor agents;
  • regulation of cell cycle

Abstract

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).