Rational design and diversity-oriented synthesis of peptoid-based selective HDAC6 inhibitors

Rational design and diversity-oriented synthesis of peptoid-based selective HDAC6 inhibitors

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 prop...

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Veröffentlicht in:Chemical communications (Cambridge, England) England), 2016-01, Vol.52 (15), p.3219-3222
Hauptverfasser: Diedrich, D, Hamacher, A, Gertzen, C. G. W, Alves Avelar, L. A, Reiss, G. J, Kurz, T, Gohlke, H, Kassack, M. U, Hansen, F. K
Format: Artikel
Sprache:eng
Schlagworte:
Drug Design
Histone Deacetylase Inhibitors - chemical synthesis
Histone Deacetylase Inhibitors - chemistry
Histone Deacetylase Inhibitors - pharmacology
Inhibitors
Libraries
Mini
Molecular Docking Simulation
Peptoids - chemistry
Selectivity
Synthesis
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Zusammenfassung: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. A mini library of selective HDAC6 inhibitors with peptoid-based cap groups was synthesized using an efficient multicomponent approach.
ISSN:1359-7345
1364-548X
DOI:10.1039/c5cc10301k