Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 243, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2022.114700
Keywords
Atropisomer; Axial chirality; Biological activity; Axial drugs; Drug discovery
Categories
Funding
- Qilu Young Scholars Program of Shandong University [SDQLQN2021-01]
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Atropisomers are axially chiral stereoisomers resulting from restricted rotation around a single bond, and they exhibit remarkable biological activity. In this review, we comprehensively summarize the bioactive compounds of atropisomers, including those bonded with C-C, C-N, and N-N bonds, and provide examples along with their biological activity.
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.
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