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. [10.1016/j.bmcl.2015.09.006]

Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors

L. Musso;R. Cincinelli
Secondo
;
S. Dallavalle
Ultimo
2015

Abstract

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.
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 CHIM/06 - Chimica Organica
Settore CHIM/08 - Chimica Farmaceutica
2015
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/336381
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