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The expanding reaction toolkit for DNA-encoded libraries
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2021-09-01 , DOI: 10.1016/j.bmcl.2021.128339
Richard J Fair 1 , Ryan T Walsh 1 , Christopher D Hupp 1
Affiliation  

Over the past decade, DNA-encoded libraries (DELs) have emerged as a leading platform for small molecule drug discovery among pharmaceutical companies, biotech companies and academic drug hunters alike. This revolutionary technology has tremendous potential that is yet to be fully realized, as the exploration of therapeutically relevant chemical space is fueled by the ever-expanding repertoire of DNA-compatible reactions used to construct the libraries. Advances in direct coupling reactions, like photo-catalytic cross couplings, unique cyclizations such as the formation of 1,2,4–oxadiazoles, and new functional group transformations are valuable contributions to the DEL reaction toolkit, and indicate where future reaction development efforts should focus in order to maximize the productivity of DELs.



中文翻译:

用于 DNA 编码文库的扩展反应工具包

在过去十年中,DNA 编码库 (DEL) 已成为制药公司、生物技术公司和学术药物猎手等小分子药物发现的领先平台。这项革命性技术具有尚未完全实现的巨大潜力,因为用于构建文库的 DNA 兼容反应的不断扩展库推动了对治疗相关化学空间的探索。直接偶联反应的进展,如光催化交叉偶联、独特的环化反应(如 1,2,4-恶二唑的形成)和新的官能团转换对 DEL 反应工具包做出了宝贵贡献,并指出了未来反应开发工作的方向专注于最大限度地提高 DEL 的生产力。

更新日期:2021-09-24
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