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

…, G Brooke, D Willows, RC Coombes, CJ Moody

Index: Vigushin, David M.; Brooke, Greg; Willows, David; Coombes, R.Charles; Moody, Christopher J. Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 21 p. 3661 - 3663

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Citation Number: 12

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 tself.