Anticancer activity evaluation of thieno[3,2-e][1,2,3]triazolo[1,5-a] pyrimidines and thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidine derivatives

Abstract

Aim. In vitro evaluation of anticancer activity of synthesized thieno[3,2-e][1,2,3]triazolo[1,5-a] pyrimidines and thieno[2,3-e][1,2,3]triazolo[1,5-a] pyrimidines. Methods. Organic synthesis, in vitro cytotoxicity assay, MTT assay, spectrophotometry, statistical analysis. Results. The isomeric thienotriazolopyrimidines synthesized were tested for their anticancer activity in the NCI-60 cancer cell line panel, a group of 60 human cancer cell lines. The selective influence of 5-oxo-4,5,6,7,8,9-hexahydrobenzo[4,5]thieno[3,2-e][1,2,3]triazolo[1,5-a]pyrimidine-3-car-boxamide on melanoma cell line SK-MEL-5 with (GP =-31,50%) was observed. Two compounds possessed a significant activity on CNS and breast cancer cells.Conclusions. Several thienotriazolopyrimidines were found to possess antitumor activity with a selective effect on a single cell line. These results are interesting for further structure optimization to increase selectivity and anticancer activity of fused pyrimidines.