BIFUNCTIONAL DEGRADERS COMPRISING ELECTROPHILIC PROTACS THAT ENGAGE DCAF1 AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME

Abstract

Disclosed are bifunctional degraders comprising electrophilic PRO-TACs that engage DCAF1 and pharmaceutical compositions comprising the same. The bifunctional degraders are of Formula A-B-C wherein, A is a ligand to a protein of interest, B is a linker that is a bond or a chemical linker that is chemically linked to A and C, and C is a ligand to the E3 ligase substrate receptor DCAF1, wherein the protein of interest is any protein having a ligand that can form a covalent bond with the linker B; and C comprises an azetidinyl acrylamide that forms a covalent bond with C1113 of DCAF1 through a Michael addition reaction.

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