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

Chemical Communications Pub Date: 2018-12-17 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.

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