Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC)

Chem Commun (Camb). 2019 Jan 17;55(7):929-932. doi: 10.1039/c8cc08716d.

Abstract

A preloaded resin consisting of a thalidomide moiety and an ethylene-oxy linker allows the simple and fast formation of PROTACs. The feasibility of the procedure was illustrated by conjugating different protein kinase inhibitors. The biological functionality of an ibrutinib-like conjugate was then confirmed by a cellular experiment.