Barceloneic acid A, a new farnesyl-protein transferase inhibitor from a Phoma species.
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.
Jayasuriya
H
H
Merck Research Laboratories, Rahway, New Jersey 07065, USA.
Ball
R G
RG
Zink
D L
DL
Smith
J L
JL
Goetz
M A
MA
Jenkins
R G
RG
Nallin-Omstead
M
M
Silverman
K C
KC
Bills
G F
GF
Lingham
R B
RB
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*
D010647:Phenyl Ethers; D012459:Salicylates; C095779:barceloneic acid A; D014166:Transferases; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase