Synthetic chalcones, flavanones, and flavones as antitumoral agents: Biological evaluation and structure–activity relationships

A series of synthetic chalcones, flavanones, and flavones has been synthesized and evaluated for antitumor activity against the human kidney carcinoma cells TK-10, human mammary adenocarcinoma cells MCF-7 (estrogen receptor-positive), and human colon adenocarcinoma cells HT-29. The most active series is the chalcone ones with the best results against TK-10 and HT-29 cells. Fourteen out of 53 analyzed compounds resulted very active against at least two of the studied tumoral cells. Alkaline single cell gel electrophoresis, comet assay, was performed as a study of the chromosomal aberrations promoted by the compounds on normal cells. Four active and two inactive chalcones were studied in the comet assay against normal human kidney cells (HK-2). A structure–activity relationship analysis of these compounds was performed and for 4- and 3,4-disubstituted derivatives a quantitative correlation was obtained in the case of anti-HT-29 activity.

A wide series of synthetic flavonoids, with druglikeness properties, were developed and evaluated as antitumoral agents against TK-10, MCF-7, and HT-29 human tumoral cells. Comet assay was performed against non-tumoral HK-2 in order to know chromosomal aberrations in normal cells. A QSAR was obtained for anti-HT-29 activities.Figure optionsDownload as PowerPoint slide