Abstract
Design, synthesis, and biological evaluation of several domains of the thiopeptide antibiotic thiostrepton led to the discovery of a biologically active fragment. The biological properties of this novel small organic molecule include antibiotic activity against methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecalis (VREF) bacterial strains, as well as cytotoxic action against a number of cancer cell lines.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Anti-Bacterial Agents / pharmacology
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Enterococcus faecalis / drug effects*
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Escherichia coli / drug effects*
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Humans
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Models, Chemical
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Peptides / pharmacology
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Plasmodium falciparum / drug effects*
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Staphylococcus / drug effects*
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Thiostrepton / chemical synthesis
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Thiostrepton / metabolism
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Thiostrepton / pharmacology*
Substances
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Anti-Bacterial Agents
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Peptides
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Thiostrepton