Synthesis and In vitro Evaluation of Triphenylethylene and Naphthalimide Derivatives for Anticancer Activity

Abstract

During last decades, cancer is emerging malignancy worldwide that accounts for the second leading cause of mortality exceeding cardiovascular disease. The incidence of cancer continues to increase in developing as well as developed countries at an alarming rate. Despite many therapeutic successes, cancer remains one of the most promising challenges in the 21st century. In the quest for potent anticancer agents, we had designed and synthesized triphenylethylene and naphthalimide analogues as potential drug candidates. These newly synthesized derivatives have been evaluated for their anticancer activity against 60 human cancer cell lines. To study the molecular targets for cytotoxicity, the effect on topoisomerase-II relaxation is reported for the most cytotoxic derivatives. Furthermore, colorimetric analysis was also performed to investigate the toxicity towards normal cell lines. The transportation behavior of human serum albumin (HSA) for the most potent analogues has also been studied with UV-Vis and fluorescence spectroscopy techniques. Docking studies were carried out for plausible explanation of the experimental biological evidences. Thus, the present work highlights the approaches employed to design and synthesize new molecular framework as therapeutic template to target TOPO-IIα for anticancer activity. Altogether, it aids medicinal chemist to develop novel drug candidates against cancer.