Regioselective one-pot synthesis and anti-proliferative and apoptotic effects of some novel tetrazolo[1,5-a]pyrimidine derivatives

An easy and efficient route for the synthesis of tetrazolopyrimidines has been achieved by the reaction 5-amino-1H-tetrazole hydrate with the sodium formyl salts of cyclic ketones as a one-step reaction, afforded in a good yield the cycloalkane ring-fused tetrazolo[1,5-a]pyrimidines. The cyclohexane ring-fused tetrazolo[1,5-a]-pyrimidine derivative, 6,7,8,9-tetrahydrotetrazolo[1,5-a] quinazoline, exhibited potential and moderate anti-proliferative effects against EAC and HepG2, respectively. These anti-tumor activities may be mediated via induction of apoptosis and cell cycle arrest.