Publication

Abstract : Cancer is a continuously adapting dynamic condition for which investigation of novel treatment strategies constitutes an integral component in its management. As part of the continuing efforts from the global community directed at eradication of cancer, we were interested in evaluating the cytotoxic potential of a series of chalcone derivatives. The study also contributes towards a preliminary understanding of the structure-activity relationship of synthetic chalcone derivatives. We screened various A-ring monosubstituted chalcone derivatives against five selected human cancer cell lines using the sulforhodamine B assay. Our in vitro observations indicated the previously established characteristic biphasic response of the chalcones. Moreover, it was found that the different substitutions at the A-ring were found to suppress the cytotoxic activity, which was evident from higher growth suppression by the unsubstituted chalcone compared to the substituted derivatives. The compound 4c exhibited similar activity to that of the unsubstituted derivative, indicating that the methyl group is not detrimental to activity. It was observed that the tested compounds were most effective on the A2780 ovarian cancer cell line exhibiting GI50 value ranging from 20-66 µM. Moreover, the analogs proved to be least cytotoxic in the HepG2 cell line with GI50 values that ranged from 39-100 µM. This study may act as a preliminary step towards understanding substituent effects on the cytotoxic activity profiles of chalcone derivatives emphasising on A-ring substituted moieties.