Synthesis and investigations into the anticancer and antibacterial activity studies of β-carboline chalcones and their bromide salts.
Synthesis and investigations into the anticancer and antibacterial activity studies of β-carboline chalcones and their bromide salts.
复制标题
DOI：
10.1016/j.bmcl.2018.03.033
复制
发表时间：
2018-05-01
影响因子：
2.7
通讯作者：
Kumar D
中科院分区：
文献类型：
--
作者：
Venkataramana Reddy PO;Hridhay M;Nikhil K;Khan S;Jha PN;Shah K;Kumar D
在碱性条件下，由容易获得的 1-乙酰基-β-咔啉和各种醛，然后使用不同的烷基溴进行 N2-烷基化，制备了一系列 16 个在 C-1 位带有查耳酮部分的 β-咔啉。评估所制备的化合物针对一组人类肿瘤细胞系的体外细胞毒性。与 N2-未取代的 β-咔啉查尔酮 12a-g 相比，N2-烷基化-β-咔啉查尔酮 13a-i 具有有趣的抗癌活性。在制备的 β-咔啉中，13g 对所有测试的癌细胞系表现出广谱活性，IC50 值低于 22.5 μM。此外，通过AO/EB染色测定，N2-烷基化-β-咔啉查耳酮13g显着诱导MDA-MB-231细胞死亡。细胞毒性最强的化合物13g具有相对较高的药物评分0.48。此外，制备的β-咔啉查尔酮对测试的细菌菌株表现出中等的抗菌活性。
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.
登录
查看更多内容
影响因子：
3.9
作者：
Reddy, Venkataramana P. O.;Tantak, Mukund P.;Kumar, Dalip
通讯作者：
Kumar, Dalip
影响因子：
2.7
作者：
Venkataramana Reddy PO;Mishra S;Tantak MP;Nikhil K;Sadana R;Shah K;Kumar D
通讯作者：
Kumar D
影响因子：
3.8
作者：
POINDEXTER, EH;CARPENTER, RD
通讯作者：
CARPENTER, RD
影响因子：
--
作者：
Ciupa, Alexander;De Bank, Paul A.;Caggiano, Lorenzo
通讯作者：
Caggiano, Lorenzo
影响因子：
3.5
作者：
Ribble, D;Goldstein, NB;Shellman, YG
通讯作者：
Shellman, YG