One-pot synthesis and cytotoxic evaluation of amide-linked 1,4-disubstituted 1,2,3-bistriazoles

A series of amide-linked 1,4-disubstituted 1,2,3-bistriazoles have been synthesized employing copper(I)-catalyzed azide-alkyne cycloaddition reaction. All the newly synthesized compounds were screened for in vitro cytotoxicity against a panel of five human cancer cell lines; Fibrosarcoma (HT-1080), Colon (colo205, HCT-116), and Lung (A549, NCIH322). Some of the bistriazoles exhibited moderate to good activity. Compounds 3n and 3o were found to be the more active and displayed broad spectrum activity against all the cancer cell lines under investigation. Further, to study the binding modes for the two more potent compounds 3n and 3o against Human topoisomerase II, docking simulations have been carried out.