DNA-encoded library technology (DELT) has made noteworthy progress on small molecule drug discovery in the past few years in the pharmaceutical industry and academia. Speaking from the small molecular libraries construction, larger chemical space can improve the success rate of affinity selection. In order to achieve these purposes, on the one hand, we explored new DNA-compatible reactions, such as C-H activation reaction, which enables many previously considered mono-functional building blocks to act like bi-functional building blocks, and contemplated that more structurally diverse DELs can be efficiently constructed; meanwhile we also developed a series of DNA compatible Heck Coupling reaction conditions that can incorporate more building blocks into DELs; on the other hand, we employed diversity-oriented-synthesis (DOS) strategy combining with DNA-compatible reactions and high-throughput experiments, to construct DELs containing spiro-, unsaturated and disubstituted scaffolds. After affinity selection, the SAR and hit molecule’s structural information can be decoded from attached DNA tags via high-throughput sequencing, which can be used as a basis for the lead optimization. 

Diversity-based DEL development and construction

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.