2. Academic Validation
  3. Identification of novel bivalent mimetics of annonaceous acetogenins via a scaffold-hopping strategy

Identification of novel bivalent mimetics of annonaceous acetogenins via a scaffold-hopping strategy

  • Bioorg Med Chem Lett. 2014 Apr 1;24(7):1650-3. doi: 10.1016/j.bmcl.2014.02.072.
Yanghan Liu 1,  Yongqiang Liu 2,  Zhen Li 3,  Guang-Biao Zhou 2,  Zhu-Jun Yao 4,  Sheng Jiang 5
Affiliations

Affiliations

  • 1 Laboratory of Medicinal Chemistry, Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, China.
  • 2 Division of Molecular Carcinogenesis and Targeted Therapy for Cancer, State Key Laboratory of Biomembrane and Membrane Biotechnology, Institute of Zoology, Chinese Academy of Sciences, Beijing 100101, China.
  • 3 Department of Translational Imaging, The Houston Methodist Research Institute, Houston, TX 77030, United States.
  • 4 State Key Laboratory of Coordination Chemistry, Nanjing National Laboratory of Microstructures, School of Chemistry and Chemical Engineering, Nanjing University, 22 Hankou Road, Nanjing 210093, China. Electronic address: yaoz@nju.edu.cn.
  • 5 Laboratory of Medicinal Chemistry, Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou 510530, China. Electronic address: jiang_sheng@gibh.ac.cn.
PMID: 24650643 DOI: 10.1016/j.bmcl.2014.02.072
Abstract

A series of novel bivalent mimetics of annonaceous acetogenins have been designed, synthesized, and evaluated. Among these, compound 7 bearing a homopiperazine ring in the middle region exhibited more potent growth inhibitory activity and higher selectivity against Cancer cells over normal cells by comparison with AA005. This work indicates that modification of the middle piperazine ring is a useful optimizing tool for the simplified acetogenin mimetics.

Keywords

Annonaceous acetogenins; Bivalent analogues; Cytotoxicity; Homopiperazine; Selectivity.

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