A series of alternative Zn-binding groups were explored in the design of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors. Most of the synthesized compounds were less effective than the parent hydroxamic acid. However, the profile of activity shown by the analog bearing a hydroxyurea head group, makes this derivative promising for further investigation.
Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors / L. Musso, R. Cincinelli, V. Zuco, F. Zunino, A. Nurisso, M. Cuendet, G. Giannini, L. Vesci, C. Pisano, S. Dallavalle. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 25:20(2015), pp. 4457-4460.
|Titolo:||Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors|
CINCINELLI, RAFFAELLA (Secondo)
DALLAVALLE, SABRINA (Ultimo) (Corresponding)
|Parole Chiave:||Antiproliferative activity; Histone deacetylase (HDAC) inhibitors; Synthesis; Zn-binding group; Biochemistry; Clinical Biochemistry; Molecular Biology; Molecular Medicine; Organic Chemistry; Drug Discovery3003 Pharmaceutical Science; 3003|
|Settore Scientifico Disciplinare:||Settore CHIM/06 - Chimica Organica|
Settore CHIM/08 - Chimica Farmaceutica
|Data di pubblicazione:||2015|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1016/j.bmcl.2015.09.006|
|Appare nelle tipologie:||01 - Articolo su periodico|