2. Academic Validation
  3. Design, synthesis, and evaluation of asymmetric EF24 analogues as potential anti-cancer agents for lung cancer

Design, synthesis, and evaluation of asymmetric EF24 analogues as potential anti-cancer agents for lung cancer

  • Eur J Med Chem. 2017 Jan 5:125:1321-1331. doi: 10.1016/j.ejmech.2016.10.027.
Jianzhang Wu 1,  Shoubiao Wu 1,  Lingyi Shi 1,  Shanshan Zhang 1,  Jiye Ren 1,  Song Yao 1,  Di Yun 1,  Lili Huang 1,  Jiabing Wang 1,  Wulan Li 2,  Xiaoping Wu 3,  Peihong Qiu 4,  Guang Liang 1
Affiliations

Affiliations

  • 1 Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical Universtiy, Wenzhou, Zhejiang 325035, China.
  • 2 Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical Universtiy, Wenzhou, Zhejiang 325035, China; College of Information Science and Computer Engineering, The First Clinical Medical College, Wenzhou Medical University, Wenzhou, Zhejiang 325035, China. Electronic address: lwlwzmu@163.com.
  • 3 Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical Universtiy, Wenzhou, Zhejiang 325035, China; Institute of Tissue Transplantation and Immunology, Key Laboratory of Functional Protein Research of Guangdong Higher Education Institutes, Key Laboratory of Molecule Immunology and Antibody Engineering of Guangdong Province, Jinan University, Guangzhou, 510632, China. Electronic address: wxpjnu@163.com.
  • 4 Chemical Biology Research Center, School of Pharmaceutical Sciences, Wenzhou Medical Universtiy, Wenzhou, Zhejiang 325035, China. Electronic address: wjzwzmc@126.com.
PMID: 27886548 DOI: 10.1016/j.ejmech.2016.10.027
Abstract

The nuclear factor-kappa B (NF-κB) signaling pathway has been targeted for the therapy of various cancers, including lung Cancer. EF24 was considered as a potent inhibitor of NF-κB signaling pathway. In this study, a series of asymmetric EF24 analogues were synthesized and evaluated for their anti-cancer activity against three lung Cancer cell lines (A549, LLC, H1650). Most of the compounds exhibited good anti-tumor activity. Among them, compound 81 showed greater cytotoxicity than EF24. Compound 81 also possessed a potent anti-migration and anti-proliferative ability against A549 cells in a concentration-dependent manner. Moreover, compound 81 induced lung Cancer cells death by inhibiting NF-κB signaling pathway, and activated the JNK-mitochondrial apoptotic pathway by increasing Reactive Oxygen Species (ROS) generation resulting in Apoptosis. In summary, compound 81 is a valuable candidate for anti-lung Cancer therapy.

Keywords

Anti-cancer activity; Asymmetric EF24 analogues; NF-κB; ROS; Synthesis.

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