Abstract
Synthesis of highly active migrastatin-based tumor migration cell inhibitors has been accomplished. Our flexible and concise total synthesis of migrastatin has allowed us to explore otherwise inaccessible migrastatin-derived structural motifs. This effort has resulted in the discovery of analogues with tumor cell migration inhibitory activity 3 orders of magnitude higher than that of the natural product.
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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Angiogenesis Inhibitors / chemical synthesis*
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Angiogenesis Inhibitors / chemistry*
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Angiogenesis Inhibitors / pharmacology
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Animals
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Cell Line, Tumor
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Cell Movement / drug effects*
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Drug Design
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Endothelium, Vascular / cytology
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Endothelium, Vascular / drug effects
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Humans
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Lactones / chemical synthesis*
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Lactones / chemistry*
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Lactones / pharmacology
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Macrolides*
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Mice
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Piperidones / chemical synthesis*
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Piperidones / chemistry*
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Piperidones / pharmacology
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Structure-Activity Relationship
Substances
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Angiogenesis Inhibitors
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Lactones
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Macrolides
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Piperidones
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migrastatin