PSL Research University, Chimie ParisTech - CNRS, Institut de Recherche de Chimie Paris, Paris, 75005, France.
Institut de Recherche Pierre Fabre, Gaillac, 81600, France.
Eur J Med Chem. 2016 Feb 15;109:287-93. doi: 10.1016/j.ejmech.2016.01.007. Epub 2016 Jan 12.
A series of new securinine analogues was prepared by Heck reaction from readily accessible securinine and commercially available iodoarenes. The in vitro cytotoxicity of the prepared compounds was assayed against a panel of four cancer cell lines: A375, A549, HCT-116 and HL-60 showing promising growth inhibition with excellent IC50 values in the nanomolar range. The plasmatic stability of the most potent analogue was also investigated demonstrating that they might serve as valuable leads for the development of anticancer drugs.
通过 Heck 反应，从易得的船底顶碱和商业可得的碘芳烃出发，制备了一系列新的船底顶碱类似物。对所制备的化合物进行了体外细胞毒性测定，针对四种癌细胞系：A375、A549、HCT-116 和 HL-60，结果显示具有优异的 IC50 值（纳摩尔范围），具有良好的生长抑制作用。还研究了最有效的类似物的血浆稳定性，表明它们可能成为开发抗癌药物的有价值的先导化合物。
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