Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases

Ambra A. Grolla, Valeria Podestà, Maria Giovanna Chini, Simone Di Micco, Antonella Vallario, Armando A. Genazzani, Pier Luigi Canonico, Giuseppe Bifulco, Gian Cesare Tron, Giovanni Sorba, Tracey Pirali

Research output: Contribution to journalArticlepeer-review

Abstract

HDAC inhibitors show great promise for the treatment of cancer. As part of a broader effort to explore the SAR of HDAC inhibitors, synthesis, biological evaluation, and molecular docking of novel Ugi products containing a zinc-chelating moiety are presented. One compound shows improved inhibitory potencies compared to SAHA, demonstrating that hindered lipophilic residues grafted on the peptide scaffold of the α-aminoacylamides can be favorable in the interaction with the enzyme.

Original languageEnglish
Pages (from-to)2776-2785
Number of pages10
JournalJournal of Medicinal Chemistry
Volume52
Issue number9
DOIs
Publication statusPublished - 14 May 2009

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