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

A series of sixteen ß-carbolines, bearing chalcone moiety at C-1 position, were prepared from easily accessible 1-acetyl-ß-carboline and various aldehydes under basic conditions followed by N2-alkylation using different alkyl bromides. The prepared compounds were evaluated for in vitro cytotoxicity against a panel of human tumor cell lines. N2-Alkylated-ß-carboline chalcones 13a-i represented the interesting anticancer activities compared to N2-unsubstituted ß-carboline chalcones 12a-g. Off the prepared ß-carbolines, 13g exhibited broad spectrum of activity with IC50 values lower than 22.5 µM against all the tested cancer cell lines. Further, the N2-alkylated-ß-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 ß-carboline chalcones displayed moderate antibacterial activities against tested bacterial strains.