Synthesis and antitumor activities of pyrimidines / 南方医科大学学报

ABSTRACT

<p><b>OBJECTIVE</b>To synthesize cyclin-dependent kinase (CDKs) inhibitors and assay their antitumor activities.</p><p><b>METHODS</b>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.</p><p><b>RESULTS</b>Their structures were characterized by MS and 1H NMR spectra and all the synthesized compounds were screened for their antimicrobial activity with MTT assay.</p><p><b>CONCLUSION</b>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.</p>