Abstract
Compounds 9 and 13 were synthesized, and their structures and stereochemistry were elucidated by spectroscopic methods. In competition binding experiments, specific [(3)H]-PGE(2) binding was significantly displaced by compound 9 and, to a lesser extent, by 13, in a dose-dependent manner. The biological properties of compound 9 were studied on HL-60 cells, and several effects were found related to those of PGE(2). Compound 9 increases c-fos mRNA level as does PGE(2) and antagonizes TPA-induced terminal differentiation.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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4-Butyrolactone / analogs & derivatives*
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4-Butyrolactone / chemical synthesis*
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4-Butyrolactone / chemistry
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4-Butyrolactone / pharmacology
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Binding, Competitive
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Cell Differentiation / drug effects
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Cell Survival / drug effects
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Dinoprostone / chemistry
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Dinoprostone / metabolism*
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HL-60 Cells
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Humans
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Proto-Oncogene Proteins c-fos / biosynthesis
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Proto-Oncogene Proteins c-fos / genetics
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RNA, Messenger / biosynthesis
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Radioligand Assay
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Stereoisomerism
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Structure-Activity Relationship
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Tetradecanoylphorbol Acetate / pharmacology
Substances
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Proto-Oncogene Proteins c-fos
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RNA, Messenger
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Dinoprostone
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Tetradecanoylphorbol Acetate
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4-Butyrolactone