Synthesis, in vitro and in silico Anti-Proliferative Studies of Novel Piperiene-Oxadiazole and Thiadiazole Analogs

Abstract

Piperine is a component of pepper which has earlier been reported as anticancer active compound. This work is emphasized on the design and synthesis of new hybrid piperine analogs by coupling piperine with the amine group of oxadiazoles and thiadiazoles. The new series of twelve piperine analogs was been tested for in vitro anti-proliferative activity using sulforhodamine B (SRB) assay test against MCF-7, PC-3, and HeLa cell lines. Among the twelve synthesised molecules piperine derivative with oxadiazole baring hydroxyl group (3) exhibits the higher activity against MCF-7 cell line than the reference drug Adriamycin and also displays the highest binding energy in the in silico studies. The other analogs are moderately active.