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
Thioethers have been widely found in biologically active compounds, including pharmaceuticals. In this report, a highly efficient approach to on-DNA construction of thioethers via Cu-promoted Ullmann cross-coupling between DNA-conjugated aryl iodides and thiols is developed. This methodology was demonstrated with medium to high yields, without obvious DNA damage. This reported reaction has strong potential for application in DNA-encoded chemical library synthesis.
Bioconjugate Chem. 2021
https://doi.org/10.1021/acs.bioconjchem.1c00076
Link:https://pubs.acs.org/doi/10.1021/acs.bioconjchem.1c00076
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