Research advances in antitumor activities of pyrimidine derivatives / 药学学报

Pyrimidine derivatives have been the subject of much attention in pesticide and medicine fields owing to their unique biological properties. Particularly, a large number of these compounds have recently been reported to show substantial antitumor activities, and some of them have been investigated in clinical trials. Although these structurally novel compounds have a common chemical moiety of a pyrimidine ring, there are a variety of mechanisms of their antitumor action, such as, inhibition of cyclin-dependent-kinases, inhibition of protein tyrosine kinase, inhibition of carbonic anhydrases, inhibition of dihydrofolate reductase and disruption of microtubule assembly. In this paper, we described the latest advances in the research of such pyrimidine derivatives as antitumor drug according to their action on targets.

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

<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>