Synthesis of pyrazolo[1,5-a]pyrimidine linked aminobenzothiazole conjugates as potential anticancer agents.
A series of pyrazolo[1,5-a]pyrimidine linked 2-aminobenzothizole conjugates (6a-t) were synthesized and evaluated for their anticancer activity against five human cancer cell lines. Among them two compounds 6p and 6m showed significant anticancer activity with IC50 values ranging from 2.01 to 7.07 and 1.94-3.46μM, respectively. Moreover, cell cycle arrest in G2/M and reduction in Cdk1 expression level were observed upon treatment of these compounds and they also induced caspase-3 dependent apoptosis. This was further confirmed by staining as well as DNA fragmentation analysis.
T1 T2 T3 T4 T5 T6
CHEMICAL CHEMICAL CHEMICAL CHEMICAL GENE-Y GENE-Y
pyrazolo[1,5-a]pyrimidine 2-aminobenzothizole pyrazolo[1,5-a]pyrimidine aminobenzothiazole Cdk1 caspase-3