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

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

  • J Med Chem. 2009 May 14;52(9):2776-85. doi: 10.1021/jm801529c.
Ambra A Grolla 1,  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
Affiliations

Affiliation

  • 1 Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche and Drug and Food Biotechnology Center, Universita degli Studi del Piemonte Orientale A. Avogadro, Via Bovio 6, 28100 Novara, Italy.
PMID: 19344175 DOI: 10.1021/jm801529c
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 alpha-aminoacylamides can be favorable in the interaction with the Enzyme.

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