A mini library of HDAC inhibitors with peptoid-based cap groups was synthesized using an efficient multicomponent approach. Four compounds were identified as potent HDAC6 inhibitors with a selectivity over other HDAC isoforms. The most potent HDAC6 inhibitor revealed remarkable chemosensitizing properties and completely reverted the cisplatin resistance in Cal27 CisR cells.
D. Diedrich, A. Hamacher, C. G. W. Gertzen, L. A. Alves Avelar, G. J. Reiss, T. Kurz, H. Gohlke, M. U. Kassack and F. K. Hansen, Chem. Commun., 2016, 52, 3219 DOI: 10.1039/C5CC10301K
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