Abstract
Novel macrocyclic peptide mimetics have been synthesized by exploiting a three-component reaction and an azide-alkyne [3 + 2] cycloaddition. The prepared compounds were screened as HDAC inhibitors allowing us to identify a new compound with promising biological activity. In order to rationalize the biological results, computational studies have also been performed.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Binding Sites
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Biomimetic Materials / chemical synthesis
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Biomimetic Materials / chemistry
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Biomimetic Materials / metabolism
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Biomimetic Materials / pharmacology
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Cell Line, Tumor
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Cell Survival / drug effects
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Dose-Response Relationship, Drug
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Drug Discovery
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Histone Deacetylase Inhibitors / chemical synthesis
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Histone Deacetylase Inhibitors / chemistry*
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Histone Deacetylase Inhibitors / metabolism
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Histone Deacetylase Inhibitors / pharmacology*
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Histone Deacetylases / chemistry
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Histone Deacetylases / metabolism
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Humans
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Models, Molecular
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Peptides, Cyclic / chemical synthesis
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Peptides, Cyclic / chemistry*
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Peptides, Cyclic / metabolism
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Peptides, Cyclic / pharmacology*
Substances
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Histone Deacetylase Inhibitors
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Peptides, Cyclic
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Histone Deacetylases