Design, synthesis and in vitro cytotoxicity studies of novel β-carbolinium bromides.
Design, synthesis and in vitro cytotoxicity studies of novel β-carbolinium bromides.
复制标题
DOI：
10.1016/j.bmcl.2017.02.010
复制
发表时间：
2017-03-15
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;Mishra S;Tantak MP;Nikhil K;Sadana R;Shah K;Kumar D
以易获得的β-碳啉和1-芳基-2-溴乙酮为原料合成了一系列新型β-碳溴化物。对新合成的化合物进行了体外抗癌活性评价。在所合成的化合物中，化合物16l、16o和16s对癌细胞的IC50值均<10 μM，具有较强的抗肿瘤活性。最有效的类似物161对所有肿瘤细胞系均有广泛的活性（IC50 = 3.16 ~ 7.93 μM）。为了测试细胞死亡的机制，我们将去势抵抗前列腺癌细胞（C4-2）暴露于化合物16l和16s中，导致裂解的PARP1和AO/EB染色水平升高，表明β-碳盐诱导这些细胞凋亡。此外，最有效的β-碳胺161和16s被发现抑制微管蛋白聚合。
A series of novel β-carbolinium bromides has been synthesized from easily accessible β-carbolines and 1-aryl-2-bromoethanones. The newly synthesized compounds were evaluated for their in vitro anticancer activity. Among the synthesized derivatives, compounds 16l, 16o and 16s exhibited potent anticancer activity with IC50 values of <10 μM against tested cancer cell lines. The most potent analogue 16l was broadly active against all the tested cancer cell lines (IC50 = 3.16–7.93 μM). In order to test the mechanism of cell death, we exposed castration resistant prostate cancer cell line (C4–2) to compounds 16l and 16s, which resulted in increased levels of cleaved PARP1 and AO/EB staining, indicating that β-carbolinium salts induce apoptosis in these cells. Additionally, the most potent β-carbolines 16l and 16s were found to inhibit tubulin polymerization.
登录
查看更多内容
影响因子：
7.3
作者：
Frederick, Raphael;Bruyere, Celine;Wouters, Johan
通讯作者：
Wouters, Johan
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：
4.1
作者：
Threadgill, Michael D.
通讯作者：
Threadgill, Michael D.
DOI：
10.1016/j.jphotobiol.2014.01.020
发表时间：
2014-03-05
影响因子：
5.4
作者：
Vignoni, Mariana;Erra-Balsells, Rosa;Cabrerizo, Franco M.
通讯作者：
Cabrerizo, Franco M.
影响因子：
3.2
作者：
Molina, Pedro;Tarraga, Alberto;Oton, Francisco
通讯作者：
Oton, Francisco