Department of Medical Experimental Center, Qilu Hospital (Qingdao), Cheeloo College of Medicine, Shandong University, Qingdao, 266035, China.
Department of Pharmacy, Qilu Hospital (Qingdao), Cheeloo College of Medicine, Shandong University, Qingdao, 266035, China.
Eur J Med Chem. 2022 Dec 5;243:114700. doi: 10.1016/j.ejmech.2022.114700. Epub 2022 Aug 28.
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.
手性轴化合物是由单键旋转受限而产生轴手性的立体异构体。这一类手性轴化合物的许多代表物对蛋白质靶标表现出显著的生物学特性。这种时变手性在药物开发方面具有巨大的潜力。本文全面综述了轴手性生物活性化合物，包括 C-C 键合的轴手性化合物、C-N 键合的轴手性化合物和 N-N 键合的轴手性化合物。每个化合物都提供了示例及其生物活性。本综述强调了在生物活性化合物中遇到的各种轴手性化合物的发展，这有利于药物化学家推进轴手性药物分子的发展。
