title: Barceloneic acid A, a new farnesyl-protein transferase inhibitor from a Phoma species.
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.
authors.affiliation: Merck Research Laboratories, Rahway, New Jersey 07065, USA.
authors.forename: H
authors.initials: H
authors.lastname: Jayasuriya
authors.forename: R G
authors.initials: RG
authors.lastname: Ball
authors.forename: D L
authors.initials: DL
authors.lastname: Zink
authors.forename: J L
authors.initials: JL
authors.lastname: Smith
authors.forename: M A
authors.initials: MA
authors.lastname: Goetz
authors.forename: R G
authors.initials: RG
authors.lastname: Jenkins
authors.forename: M
authors.initials: M
authors.lastname: Nallin-Omstead
authors.forename: K C
authors.initials: KC
authors.lastname: Silverman
authors.forename: G F
authors.initials: GF
authors.lastname: Bills
authors.forename: R B
authors.initials: RB
authors.lastname: Lingham
mesh_terms: D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase; D005285:Fermentation; D011905:Genes, ras / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008745:Methylation; D010084:Oxidation-Reduction; D010647:Phenyl Ethers / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D012459:Salicylates / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D014166:Transferases / Q000037:antagonists & inhibitors*; D014961:X-Ray Diffraction; D013098:Xylariales / Q000378:metabolism*
chemical_list: D010647:Phenyl Ethers; D012459:Salicylates; C095779:barceloneic acid A; D014166:Transferases; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase