Abstract
Inhibitors of histone deacetylases (HDACs) are a promising class of anticancer agents that effect gene regulation. To know the interaction of aliphatic cap groups with HDACs, cyclic tetrapeptide and bicyclic peptide disulfide hybrids were synthesized without aromatic ring in their macrocyclic framework. Benzene ring of l-Phe in chlamydocin was replaced with several aliphatic amino acids and also a fused bicyclic tetrapeptide was synthesized by ring closing metathesis using Grubb's first generation catalyst. The inhibitory activities of the cyclic peptides against histone deacetylase enzymes were evaluated, which demonstrated most of them are interesting candidates as anticancer agents.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Cell Line
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacology
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Histone Deacetylase 1
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Histone Deacetylase 6
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Histone Deacetylase Inhibitors*
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Histone Deacetylases
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Humans
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Inhibitory Concentration 50
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Peptides, Cyclic / chemical synthesis*
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Peptides, Cyclic / pharmacology*
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Repressor Proteins
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Histone Deacetylase Inhibitors
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Peptides, Cyclic
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Repressor Proteins
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HDAC1 protein, human
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HDAC4 protein, human
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HDAC6 protein, human
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Histone Deacetylase 1
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Histone Deacetylase 6
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Histone Deacetylases