2. Academic Validation
  3. Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors

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

  • Bioorg Med Chem Lett. 2015 Oct 15;25(20):4457-60. doi: 10.1016/j.bmcl.2015.09.006.
Loana Musso 1,  Raffaella Cincinelli 1,  Valentina Zuco 2,  Franco Zunino 2,  Alessandra Nurisso 3,  Muriel Cuendet 3,  Giuseppe Giannini 4,  Loredana Vesci 4,  Claudio Pisano 4,  Sabrina Dallavalle 5
Affiliations

Affiliations

  • 1 Department of Food, Environmental and Nutritional Sciences, University of Milan, Via Celoria 2, 20133 Milan, Italy.
  • 2 Fondazione IRCCS Istituto Nazionale Tumori, Via Amadeo 42, 20133 Milan, Italy.
  • 3 School of Pharmaceutical Sciences, University of Geneva, University of Lausanne, Quai Ernest-Ansermet 30, 1211 Geneva 11, Switzerland.
  • 4 R&D Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Via Pontina Km 30,400, I-00040 Pomezia, Roma, Italy.
  • 5 Department of Food, Environmental and Nutritional Sciences, University of Milan, Via Celoria 2, 20133 Milan, Italy. Electronic address: sabrina.dallavalle@unimi.it.
PMID: 26376355 DOI: 10.1016/j.bmcl.2015.09.006
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.

Keywords

Antiproliferative activity; Histone deacetylase (HDAC) inhibitors; Synthesis; Zn-binding group.

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