[Synthesis and antitumor activities of pyrimidines].

Abstract

To synthesize cyclin-dependent kinase (CDKs) inhibitors and assay their antitumor activities. A series of pyrimidines containing different arylamino and 1-(methylsulfonyl)piperidin moieties were designed by combining the segments 1-(methylsulfonyl)piperidin and pyrimidine heterocycles according to the super-position principle of the reinforcement of biological activities. Their structures were characterized by MS and 1H NMR spectra and all the synthesized compounds were screened for their antimicrobial activity with MTT assay. The preliminary bioassay showed that compound 3 b displayed good antitumor activity (IC(50)=13.6 μmol/L). The preliminary structure activity relationship analysis of these analogues suggest that the steric factor may have important impact on the anti-tumor activity.