Design and synthesis of pregnenolone/2-cyanoacryloyl conjugates with dual NF-kappa B inhibitory and anti-proliferative activities

文献类型： 外文期刊

第一作者： Song, Jia-Li

作者： Song, Jia-Li;Zhu, Kong-Kai;Yang, Fei-Fei;Liu, Xi-Gong;Zhang, Yu-Ying;Jiang, Cheng-Shi;Zhang, Hua;Zhang, Juan;Longo, Joao Paulo Figueiro;Muehlmann, Luis Alexandre;Zhang, Juan;Longo, Joao Paulo Figueiro;Muehlmann, Luis Alexandre;Azevedo, Ricardo Bentes;Liu, Chang-Liang;Liu, Chao;Guo, Yue-Wei

作者机构：

关键词： Pregnenolone; NF-kappa B; 2-Cyanoacryloyl; Michael acceptor; Anti-proliferative activity

期刊名称：BIOORGANIC & MEDICINAL CHEMISTRY LETTERS （ 影响因子：2.823； 五年影响因子：2.677 ）

ISSN： 0960-894X

年卷期： 2017 年 27 卷 20 期

页码：

收录情况： SCI

摘要： Twenty-five novel pregnenolone/2-cyanoacryloyl conjugates (6-30) were designed and prepared, with the aim of developing novel anticancer drugs with dual NF-kappa B inhibitory and anti-proliferative activities. Compounds 22 and 27-30 showed inhibition against TNF-alpha-induced NF-kappa B activation in luciferase assay, which was confirmed by Western blotting. Among them, compound 30 showed potent NF-kappa B inhibitory activity (IC50 = 2.5 mu M) and anti-proliferative against MCF-7, A549, H157, and HL-60 cell lines (IC50 = 6.5-36.2 mu M). The present study indicated that pregnenolone/2-cyanoacryloyl conjugate I can server as a novel scaffold for developing NF-kappa B inhibitors and anti-proliferative agents in cancer chemotherapy. (C) 2017 Elsevier Ltd. All rights reserved.

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