A series of sixteen β-carbolines, bearing chalcone moiety at C-1 position, were prepared from easily accessible 1-acetyl-β-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-β-carboline chalcones 13a-i represented the interesting anticancer activities compared to N²-unsubstituted β-carboline chalcones 12a-g. Off the prepared β-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-β-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 β-carboline chalcones displayed moderate antibacterial activities against tested bacterial strains.

在碱性条件下，由易得的1-乙酰基-β-咔啉和各种醛制备一系列十六个在C-1位带有查耳酮部分的β-咔啉，然后使用不同的烷基溴进行N ^2-烷基化。评价了所制备的化合物对一组人类肿瘤细胞系的体外细胞毒性。Ñ ²烷基化-β咔啉查耳酮13A-I表示的有趣抗癌活性相比Ñ ² -未被取代的β咔啉查耳酮12A-G 。在制备的β-咔啉中，13g的IC ₅₀表现出广谱的活性对于所有测试的癌细胞系，其值均低于22.5 µM。此外，通过AO / EB染色测定法，N ^2-烷基化-β-咔啉查尔酮13g在MDA-MB-231细胞中明显诱导细胞死亡。具有最高细胞毒性的化合物13g的药物得分较高，为0.48。另外，制备的β-咔啉查耳酮对测试的细菌菌株显示出中等的抗菌活性。