This review profiles twelve fluorine-containing drugs approved by the US Food and Drug Administration(FDA) for the clinic in 2023.These small molecule drugs represent such therapeutic areas as cancer,neuromuscular dis...This review profiles twelve fluorine-containing drugs approved by the US Food and Drug Administration(FDA) for the clinic in 2023.These small molecule drugs represent such therapeutic areas as cancer,neuromuscular disorder,immunodeficiency,virology,and infectious diseases.Medicinal chemistry discovery,biological activity,and synthetic routes have been discussed for each drug.Also,new trends in structural positioning,functionality,and degree of fluorination are discussed.Besides fluorination,the importance of amino acid residues and chirality in the design of new pharmaceuticals is highlighted.展开更多
基金support from the National Natural Science Foundation of China (No.21761132021)the Qing-Lan Project of Jiangsu Province (for Han) and IKERBASQUE,Basque Foundation for Science (for Soloshonok)。
文摘This review profiles twelve fluorine-containing drugs approved by the US Food and Drug Administration(FDA) for the clinic in 2023.These small molecule drugs represent such therapeutic areas as cancer,neuromuscular disorder,immunodeficiency,virology,and infectious diseases.Medicinal chemistry discovery,biological activity,and synthetic routes have been discussed for each drug.Also,new trends in structural positioning,functionality,and degree of fluorination are discussed.Besides fluorination,the importance of amino acid residues and chirality in the design of new pharmaceuticals is highlighted.