SYNTHESIS OF STEROIDAL 1,2,4TRIAZOLO1,5-aPYRIMIDINES AND THEIR ANTIPROLIFERATIVE ACTIVITIES

摘要

A facile strategy for the synthesis of steroidal 1,2,4triazolo1,5-apyrimidines 5a-g and 6a-g has been accomplished via a one-pot reaction of steroidal ketones, aromatic aldehydes and 3-amino-1,2,4-triazole in the presence of potassium tert-butoxide in refluxing tert-butanol. All the synthesized heterosteroids were evaluated for in vitro antiproliferative activity against human cancer cells by sulforhodamine B (SRB) assays. The preliminary results showed that compounds 6a and 6e possessed potent antiproliferative activities.