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

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

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: lizhong@ecust.edu.cn.
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.

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