Bioorg Med Chem Lett. 2003 Nov 3;13(21):3661-3.

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

Vigushin DM, Brooke G, Willows D, Coombes RC, Moody CJ.

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Department of Cancer Medicine, 6th Floor MRC Cyclotron Building, Imperial College of Science, Technology and Medicine, Hammersmith Hospital Campus, Du Cane Road, London W12 0NN, UK. d.vigushin@imperial.ac.uk

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 itself.

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Pyrazino[1,2-a]indole-1,4-diones, simple analogues of gliotoxin, as selective in...
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