Huang Qianping, Gu Yuang, Qin An, Ma Peixiang, Xu Hongtao, Zhang Shuning
Shanghai Institute for Advanced Immunochemical Studies (SIAIS), ShanghaiTech University, Shanghai 201210, P.R. China.
Shanghai Key Laboratory of Orthopedic Implants, Department of Orthopedics, Shanghai Ninth People's Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200025, P.R. China.
ACS Med Chem Lett. 2024 Aug 23;15(9):1591-1597. doi: 10.1021/acsmedchemlett.4c00307. eCollection 2024 Sep 12.
DNA-encoded library (DEL) is a powerful hit selection technique in both basic science and innovative drug discovery. In this study, we report a robust and straightforward DNA-compatible diazo-transfer reaction utilizing FSON as the diazo-transfer reagent in solution. This reaction demonstrates high conversions and facile operation while being metal-free and maintaining high levels of DNA fidelity. It is also compatible with a wide range of substrates, allowing for convenient access to both aliphatic and aromatic amines. Consequently, it will further enrich the DEL chemistry toolbox.
DNA编码文库（DEL）在基础科学和创新药物发现中都是一种强大的命中筛选技术。在本研究中，我们报道了一种稳健且简便的与DNA兼容的重氮转移反应，该反应在溶液中使用FSON作为重氮转移试剂。此反应转化率高、操作简便，无需金属且能保持高水平的DNA保真度。它还与多种底物兼容，便于制备脂肪族和芳香族胺。因此，它将进一步丰富DEL化学工具箱。
