Bioactive atropisomers: Unraveling design strategies and synthetic routes for drug discovery

Shuai-Jiang Liu; Qian Zhao; Xiao-Chen Liu; Allan B. Gamble; Wei Huang; Qian-Qian Yang; Bo Han

doi:10.1002/med.22037

Bioactive atropisomers: Unraveling design strategies and synthetic routes for drug discovery

Shuai-Jiang Liu, Qian Zhao, Xiao-Chen Liu, Allan B. Gamble, Wei Huang, Qian-Qian Yang Bo Han

Medicinal research reviews, Vol.44(5), pp.1971-2014

21/03/2024

: https://doi.org/10.1002/med.22037

https://hdl.handle.net/10523/24067

atropisomerism

design strategies

rotational barrier

structure‐function relationship

synthetic routes

Atropisomerism, an expression of axial chirality caused by limited bond rotation, is a prominent aspect within the field of medicinal chemistry. It has been shown that atropisomers of a wide range of compounds, including established FDA-approved drugs and experimental molecules, display markedly different biological activities. The time-dependent reversal of chirality in atropisomers poses complexity and obstacles in the process of drug discovery and development. Nonetheless, recent progress in understanding atropisomerism and enhanced characterization methods have greatly assisted medicinal chemists in the effective development of atropisomeric drug molecules. This article provides a comprehensive review of their special design thoughts, synthetic routes, and biological activities, serving as a reference for the synthesis and biological evaluation of bioactive atropisomers in the future.

Inside Front Cover Image, Volume 44, Issue 5

: 9926514746701891
: Bioactive atropisomers: Unraveling design strategies and synthetic routes for drug discovery
: Shuai-Jiang Liu
Qian Zhao
Xiao-Chen Liu
Allan B. Gamble
Wei Huang
Qian-Qian Yang
Bo Han
: School of Pharmacy and Pharmacology
: Medicinal research reviews, Vol.44(5), pp.1971-2014
: Wiley
: 21/03/2024
: National Natural Science Foundation of China (82374155, 82374020 and 22107015); Innovation Team and Talents Cultivation Program of National Administration of Traditional Chinese Medicine (ZYYCXTD-D-202209); New Zealand–China Non-Communicable Diseases Research Collaboration Centre
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: English
: Journal article