Pyrazino[1,2-a]indole-1,4-diones, simple analogues of gliotoxin, as selective inhibitors of geranylgeranyltransferase I

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...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-11, Vol.13 (21), p.3661-3663
Hauptverfasser:	VIGUSHIN, David M, BROOKE, Greg, WILLOWS, David, COOMBES, R. Charles, MOODY, Christopher J
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkyl and Aryl Transferases - antagonists & inhibitors Antineoplastic agents Biological and medical sciences Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Farnesyltranstransferase General aspects Genes, ras - genetics Gliotoxin - analogs & derivatives Gliotoxin - pharmacology Indoles - chemical synthesis Indoles - pharmacology Medical sciences Pharmacology. Drug treatments Pyrazines - chemical synthesis Pyrazines - pharmacology Recombinant Proteins - chemical synthesis Recombinant Proteins - pharmacology Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2003.08.022