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

  • Bioorg Med Chem Lett. 2014 Aug 15;24(16):3948-51. doi: 10.1016/j.bmcl.2014.06.041.
Yinbo Chen  1 ,  Vanminh Le  1 ,  Xiaoyong Xu  1 ,  Xusheng Shao  1 ,  Jianwen Liu  1 ,  Zhong Li  2
Affiliations
  • 1. Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
  • 2. Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China. Electronic address: [email protected].
PMID: 25017036 DOI: 10.1016/j.bmcl.2014.06.041
Abstract

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.

Keywords
1,5-Benzodiazepine-2,4-dione; Anthranilic diamide; Antitumor activity; Conformational restriction; Synthesis.