Abstract
To enable studies to elucidate the intracellular processing and targeting of the potent cytostatic/apoptotic anticancer natural products phorboxazoles A and B, a fluorescent derivative has been developed. This involved the total syntheses of the terminal alkyne 33-O-Me-45,46-dehydrobromophorboxazole A (MDHBPA) and a terminal vinyl iodide derivative of the blue fluorescent dye N,N,-dimethyl-7-aminocoumarin (DMC). Sonogashira coupling of these partners provided enyne DMC-MDHBPA in high yield.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Aminocoumarins / chemical synthesis
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Aminocoumarins / chemistry
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Aminocoumarins / pharmacology
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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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Cell Line, Tumor
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Cell Proliferation / drug effects
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Drug Design
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Drug Screening Assays, Antitumor
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Fluorescent Dyes* / chemical synthesis
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Fluorescent Dyes* / chemistry
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Fluorescent Dyes* / pharmacology
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Heterocyclic Compounds, 4 or More Rings* / chemical synthesis
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Heterocyclic Compounds, 4 or More Rings* / chemistry
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Heterocyclic Compounds, 4 or More Rings* / pharmacology
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Humans
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Molecular Conformation
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Oxazoles* / chemical synthesis
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Oxazoles* / chemistry
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Oxazoles* / pharmacology
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Structure-Activity Relationship
Substances
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Aminocoumarins
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Antineoplastic Agents
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Fluorescent Dyes
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Heterocyclic Compounds, 4 or More Rings
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Oxazoles
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phorboxazole A