HitGen has established a drug discovery research platform for small molecules and nucleic acid drugs centered on the design, synthesis and screening of DNA encoded chemical libraries (DELs), fragment-based drug discovery (FBDD) and structure-based drug design (SBDD) technologies.
Abstract:
A DNA‐encoded chemical library (DECL) is built with combinatorial chemistry, which works by bringing chemical fragments together to generate diverse structures. However, chemical diversity of DNA‐encoded chemical libraries is often limited by DNA compatible synthetic reactions. This report shows a conceptual strategy to expand chemical space of DNA‐encoded chemical libraries by incorporation of diversity‐oriented synthesis in DECL synthesis. We developed Aldol reactions on DNA in a combinatorial way. After obtaining DNA‐tagged α, β‐unsaturated ketones which represent important chemical intermediates, many distinct structures with skeletal diversities are achieved by diversity‐oriented synthesis.
Chem. Asian J. 2020, 15, 4033.
https://doi.org/10.1002/asia.202001105
Link:https://onlinelibrary.wiley.com/action/showCitFormats?doi=10.1002%2Fasia.202001105