Abstract
Some pyrazino[1,2-a]indole-1,4-diones, structurally simplified analogues of the natural mycotoxin gliotoxin, have been synthesised and investigated as inhibitors of prenyltransferases; one compound, 3-acetylthio-9-methoxy-2-methyl-2,3-dihydropyrazino[1,2-a]indole-1,4-dione 10 shows slightly greater selectivity (8-fold) for geranylgeranyltransferase type I (GGTase I) than gliotoxin itself.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkyl and Aryl Transferases / antagonists & inhibitors*
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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Farnesyltranstransferase
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Genes, ras / genetics
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Gliotoxin / analogs & derivatives*
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Gliotoxin / pharmacology*
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Indoles / chemical synthesis*
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Indoles / pharmacology*
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Pyrazines / chemical synthesis*
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Pyrazines / pharmacology*
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Recombinant Proteins / chemical synthesis
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Recombinant Proteins / pharmacology
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Indoles
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Pyrazines
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Recombinant Proteins
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Gliotoxin
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Alkyl and Aryl Transferases
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geranylgeranyltransferase type-I
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Farnesyltranstransferase