Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC)
2019
Krajcovicova, S. | Jorda, R. | Hendrychova, D. | Krystof, V. | Soural, M.
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.
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