文献类型：期刊文献

英文题名：Discovery of novel 1,5-benzodiazepine-2,4-dione derivatives as potential anticancer agents

作者：Chen, Yinbo[1];Le, Vanminh[1];Xu, Xiaoyong[1];Shao, Xusheng[1];Liu, Jianwen[1];Li, Zhong[1]

机构：[1]E China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab Chem Biol, Shanghai 200237, Peoples R China

年份：2014

卷号：24

期号：16

起止页码：3948

外文期刊名：BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000340565900052)】；

基金：This work was financially supported by the National Basic Research Program of China (973 Program, 2010CB126100), the National High Technology Research and Development Program of China (863 Program, 2011AA10A207), and the National Natural Science Foundation of China (21372079, 21272071). This work was also partly supported by the National Key Technology R&D Program of China (2011BAE06B01) and the Fundamental Research Funds for the Central Universities.

语种：英文

外文关键词：1,5-Benzodiazepine-2,4-dione; Anthranilic diamide; Conformational restriction; Synthesis; Antitumor activity

摘要：A series of novel 1,5-benzodiazepine-2,4-dione derivatives with C-6 amide substituents were designed and synthesized using three-component reactions. The preliminary assays showed that most of them displayed moderate to good antitumor activities against human lung carcinoma (A549), human breast epithelial carcinoma (MCF-7), human colon carcinoma (HCT116), human cervical carcinoma (Hela) and Lewis lung carcinoma (2LL). Exhilaratingly, the activity level of 6m rivaled that of 5-Fluorouracil (5-Fu) against MCF-7 cell lines, which might be used as novel lead scaffold for potential anticancer development. (C) 2014 Elsevier Ltd. All rights reserved.