Abstract
Three new diphenyl ethers, barceloneic acids A, B, and barceloneic lactone [1, 2, and 3, respectively] were isolated from a fermentation extract of a fungus of the genus Phoma. The structures of compounds 1-3 were determined by a combination of spectroscopic and single-crystal X-ray diffraction methods. The effect of these compounds on the inhibition of farnesyl-protein transferase (FPTase) was evaluated and results are presented. Barceloneic acid A [1] is a novel and modest inhibitor of FPTase with an IC50 value of 40 microM.
MeSH terms
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Alkyl and Aryl Transferases*
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Farnesyltranstransferase
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Fermentation
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Genes, ras / drug effects
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Magnetic Resonance Spectroscopy
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Mass Spectrometry
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Methylation
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Oxidation-Reduction
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Phenyl Ethers / chemistry
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Phenyl Ethers / isolation & purification*
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Phenyl Ethers / pharmacology
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Salicylates / chemistry
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Salicylates / isolation & purification*
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Salicylates / pharmacology
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Transferases / antagonists & inhibitors*
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X-Ray Diffraction
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Xylariales / metabolism*
Substances
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Phenyl Ethers
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Salicylates
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barceloneic acid A
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Transferases
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Alkyl and Aryl Transferases
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Farnesyltranstransferase