title: Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases.
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.
authors.affiliation: 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.
authors.forename: Ambra A
authors.initials: AA
authors.lastname: Grolla
authors.forename: Valeria
authors.initials: V
authors.lastname: Podestà
authors.forename: Maria Giovanna
authors.initials: MG
authors.lastname: Chini
authors.forename: Simone
authors.initials: S
authors.lastname: Di Micco
authors.forename: Antonella
authors.initials: A
authors.lastname: Vallario
authors.forename: Armando A
authors.initials: AA
authors.lastname: Genazzani
authors.forename: Pier Luigi
authors.initials: PL
authors.lastname: Canonico
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Bifulco
authors.forename: Gian Cesare
authors.initials: GC
authors.lastname: Tron
authors.forename: Giovanni
authors.initials: G
authors.lastname: Sorba
authors.forename: Tracey
authors.initials: T
authors.lastname: Pirali