Abstract
[reaction: see text] Amamistatins A and B are natural products found to have anti-proliferative effects against MCF-7, A549, and MKN45 human tumor cell lines (IC50 0.24-0.56 microM). It was proposed that their activity was due to histone deacetylase (HDAC) inhibition mediated by the N-formyl-N-hydroxy lysine moiety. Amamistatin B fragment analogs were synthesized and screened for biological activity. These compounds were modest HDAC inhibitors and showed antitumor activity against MCF-7 and PC-3 human tumor cells.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Biological Products / chemistry
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Histone Deacetylase Inhibitors*
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Histone Deacetylases / metabolism
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Humans
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Hydroxamic Acids / chemistry
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Molecular Structure
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Oligopeptides / chemical synthesis*
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Oligopeptides / chemistry
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Oligopeptides / pharmacology*
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Oxazoles / chemical synthesis*
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Oxazoles / chemistry
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Oxazoles / pharmacology*
Substances
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Antineoplastic Agents
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Biological Products
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Histone Deacetylase Inhibitors
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Hydroxamic Acids
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Oligopeptides
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Oxazoles
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amamistatin A
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amamistatin B
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Histone Deacetylases