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Clickable Selenylation – a Paradigm for Seleno‐Medicinal Chemistry

Von Wiley-VCH zur Verfügung gestellt

Selenium is an emerging versatile player in medicinal chemistry, however, the research on org-Se therapeutic agents is still in its infancy due to lack of efficient selenylation chemistry. To circumvent the lack of efficient methods for the synthesis of org-Se library, the concept of clickable selenylation was proposed for their practical application in parallel library and DNA-encoded library synthesis.


Abstract

Selenium (Se) is an emerging versatile player in medicinal chemistry. The incorporation of Se into small molecules and natural products could have multiple benefits. However, the lack of efficient methods for the synthesis of Se-containing chemical library has greatly hindered the development of seleno-medicinal chemistry. With the aim to address this issue, we proposed the development of “clickable selenylation” reactions, which can be used in the synthesis of Se-containing in situ library and DNA-encoded library (SeDEL), thereby quickly producing ultra-large collections of Se-containing compounds and boosting the development of seleno-medicinal chemistry. This research paradigm can be concluded as “clickable selenylation chemistry development→in situ library construction/SeDEL synthesis→phenotype- or target-based screening→seleno-hit compound”.

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