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  3. Recent progress toward developing axial chirality bioactive compounds

Recent progress toward developing axial chirality bioactive compounds

  • Eur J Med Chem. 2022 Dec 5:243:114700. doi: 10.1016/j.ejmech.2022.114700.
Zheyi Wang 1,  Liying Meng 1,  Xinxin Liu 1,  Lingzi Zhang 2,  Zongjiang Yu 3,  Guanzhao Wu 4
Affiliations

Affiliations

  • 1 Department of Medical Experimental Center, Qilu Hospital (Qingdao), Cheeloo College of Medicine, Shandong University, Qingdao, 266035, China.
  • 2 Department of Pharmacy, Qilu Hospital (Qingdao), Cheeloo College of Medicine, Shandong University, Qingdao, 266035, China.
  • 3 CAS Key Laboratory of Bio-based Materials, Qingdao Institute of BioEnergy and Bioprocess Technology, Chinese Academy of Sciences, Qingdao, 266101, People's Republic of China. Electronic address: yuzj@qibebt.ac.cn.
  • 4 Department of Medical Experimental Center, Qilu Hospital (Qingdao), Cheeloo College of Medicine, Shandong University, Qingdao, 266035, China. Electronic address: guanzhao.wu@email.sdu.edu.cn.
PMID: 36058089 DOI: 10.1016/j.ejmech.2022.114700
Abstract

Atropisomers are stereoisomers with axial chirality arising from restricted rotation around a single bond. Lots of representatives of this class of axially chiral compounds exhibit remarkable biological properties for protein targets. This time-dependent chirality shows great potential for drug development. Herein, we comprehensively review axial chirality bioactive compounds, including C-C bonded atropisomers, C-N bonded atropisomers, and N-N bonded atropisomers. Examples of each are provided along with their biological activity. This review highlights the development of various examples of atropisomerism encountered in bioactive compounds, which is beneficial for medicinal chemists to advance atropisomeric drug molecules.

Keywords

Atropisomer; Axial chirality; Axial drugs; Biological activity; Drug discovery.

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