Synthesis and investigations into the anticancer and antibacterial activity studies of ?-carboline chalcones and their bromide salts.

A series of sixteen ?-carbolines, bearing chalcone moiety at C-1 position, were prepared from easily accessible 1-acetyl-?-carboline and various aldehydes under basic conditions followed by N-alkylation using different alkyl bromides. The prepared compounds were evaluated for in vitro cytotoxicity against a panel of human tumor cell lines. N-Alkylated-?-carboline chalcones 13a-i represented the interesting anticancer activities compared to N-unsubstituted ?-carboline chalcones 12a-g. Off the prepared ?-carbolines, 13g exhibited broad spectrum of activity with IC values lower than 22.5?µM against all the tested cancer cell lines. Further, the N-alkylated-?-carboline chalcone 13g markedly induced cell death in MDA-MB-231 cells by AO/EB staining assay. The most cytotoxic compound 13g possessed a relatively high drug score of 0.48. Additionally, the prepared ?-carboline chalcones displayed moderate antibacterial activities against tested bacterial strains.