Investigation on the ZBG-functionality of phenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase inhibitors.
- Musso L Department of Food, Environmental and Nutritional Sciences, University of Milan, Via Celoria 2, 20133 Milan, Italy.
- Cincinelli R Department of Food, Environmental and Nutritional Sciences, University of Milan, Via Celoria 2, 20133 Milan, Italy.
- Zuco V Fondazione IRCCS Istituto Nazionale Tumori, Via Amadeo 42, 20133 Milan, Italy.
- Zunino F Fondazione IRCCS Istituto Nazionale Tumori, Via Amadeo 42, 20133 Milan, Italy.
- Nurisso A School of Pharmaceutical Sciences, University of Geneva, University of Lausanne, Quai Ernest-Ansermet 30, 1211 Geneva 11, Switzerland.
- Cuendet M School of Pharmaceutical Sciences, University of Geneva, University of Lausanne, Quai Ernest-Ansermet 30, 1211 Geneva 11, Switzerland.
- Giannini G R&D Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Via Pontina Km 30,400, I-00040 Pomezia, Roma, Italy.
- Vesci L R&D Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Via Pontina Km 30,400, I-00040 Pomezia, Roma, Italy.
- Pisano C R&D Sigma-Tau Industrie Farmaceutiche Riunite S.p.A., Via Pontina Km 30,400, I-00040 Pomezia, Roma, Italy.
- Dallavalle S Department of Food, Environmental and Nutritional Sciences, University of Milan, Via Celoria 2, 20133 Milan, Italy. Electronic address: sabrina.dallavalle@unimi.it.
- 2015-09-17
Published in:
- Bioorganic & medicinal chemistry letters. - 2015
Antiproliferative activity
Histone deacetylase (HDAC) inhibitors
Synthesis
Zn-binding group
Cell Line, Tumor
Cell Proliferation
Dose-Response Relationship, Drug
Histone Deacetylase 2
Histone Deacetylase Inhibitors
Humans
Hydroxamic Acids
Models, Molecular
Molecular Structure
Organometallic Compounds
Structure-Activity Relationship
Zinc
English
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.
- Language
-
- English
- Open access status
- green
- Identifiers
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- DOI 10.1016/j.bmcl.2015.09.006
- PMID 26376355
- Persistent URL
- https://folia.unifr.ch/global/documents/109038
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