Synthesis and Antitumor Activity Evaluation of Novel Substituted 5H-Benzo[i][1,3,4]thiadiazolo[3,2-a]quinazoline-6,7-diones.

A series of novel substituted 5H-benzo[i][1,3,4]thiadiazolo[3,2-a]quinazoline-6,7-diones, designed via a molecular hybridization approach, were synthesized in very good yields using one-pot condensation of 2-hydroxy-1,4-naphthoquinone, aldehydes, and 5-substituted-2-amino-1,3,4-thiadiazole. The antitumor activities of all the synthesized compounds were assessed on two different human cancer cell lines (HCT116 and HepG2), and the results showed that most of the new compounds showed good to potent cytotoxic activities.