Issue 7, 2019
From the journal:

Chemical Communications

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

S. Krajcovicova, ORCID logo a   R. Jorda, ORCID logo b   D. Hendrychova, ORCID logo b   V. Krystof ORCID logo *b  and  M. Soural ORCID logo *c  

* Corresponding authors

a Department of Organic Chemistry, Faculty of Science, Palacky University, 17. listopadu 12, 771 46 Olomouc, Czech Republic

b Laboratory of Growth Regulators, Palacky University & Institute of Experimental Botany, the Czech Academy of Sciences, Slechtitelu 27, 78371 Olomouc, Czech Republic
E-mail: vladimir.krystof@upol.cz

c Institute of Molecular and Translational Medicine, Faculty of Medicine and Dentistry, Palacky University, Hnevotinska 5, 779 00, Olomouc, Czech Republic
E-mail: miroslav.soural@upol.cz

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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Article information

DOI
https://doi.org/10.1039/C8CC08716D
Article type
Communication
Submitted
01 Nov 2018
Accepted
17 Dec 2018
First published
17 Dec 2018

Chem. Commun., 2019,55, 929-932

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

S. Krajcovicova, R. Jorda, D. Hendrychova, V. Krystof and M. Soural, Chem. Commun., 2019, 55, 929 DOI: 10.1039/C8CC08716D

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