Abstract
A series of simplified discodermolide analogues have been designed and synthesized in an attempt to understand the role of the lactone ring. These synthetic efforts have led to an unsubstituted butyrolactone 9 being generated, which shows improved activity over the natural product.
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.
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Alkanes / chemistry*
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Alkanes / pharmacology*
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Antineoplastic Agents / chemistry*
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Antineoplastic Agents / pharmacology*
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Carbamates / chemistry*
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Carbamates / pharmacology*
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Cell Line, Tumor
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Drug Screening Assays, Antitumor
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Humans
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Lactones / chemistry*
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Lactones / pharmacology*
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Molecular Conformation
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Pyrones
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Alkanes
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Antineoplastic Agents
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Carbamates
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Lactones
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Pyrones
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discodermolide