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.

阻转异构体是具有轴向手性的立体异构体，由围绕单键的受限旋转产生。这类轴向手性化合物的许多代表对蛋白质靶标表现出显着的生物学特性。这种时间依赖性手性显示出药物开发的巨大潜力。在此，我们全面回顾了轴向手性生物活性化合物，包括 C-C 键合阻转异构体、C-N 键合阻转异构体和 N-N 键合阻转异构体。提供了每一种的例子以及它们的生物活性。这篇综述重点介绍了生物活性化合物中遇到的各种阻转异构例子的发展，这有利于药物化学家推进阻转异构药物分子的发展。