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