In-solution direct oxidative coupling for the integration of sulfur/selenium into DNA-encoded chemical libraries.

ABSTRACT: Sulfur/selenium-containing electron-rich arenes (ERAs) exist in a wide range of both approved and investigational drugs with diverse pharmacological activities. These unique chemical structures and bioactive properties, if combined with the emerging DNA-encoded chemical library (DEL) technique, would facilitate drug and chemical probe discovery. However, it remains challenging, as there is no general DNA-compatible synthetic methodology available for the formation of C-S and C-Se bonds in aqueous solution. Herein, an in-solution direct oxidative coupling procedure that could efficiently integrate sulfur/selenium into the ERA under mild conditions is presented. This method features simple DNA-conjugated electron-rich arenes with a broad substrate scope and a transition-metal free process. F

SUBMITTER: Yang S 

PROVIDER: S-EPMC8890091 | biostudies-literature | 2022 Mar

REPOSITORIES: biostudies-literature