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

Vigushin, David M and Brooke, Greg and Willows, David and Coombes, R Charles and Moody, Christopher J (2003) 'Pyrazino[1,2- a ]indole-1,4-diones, simple analogues of gliotoxin, as selective inhibitors of geranylgeranyltransferase I.' Bioorganic & Medicinal Chemistry Letters, 13 (21). pp. 3661-3663. ISSN 0960-894X

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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. © 2003 Elsevier Ltd. All rights reserved.

Item Type: Article
Uncontrolled Keywords: Pyrazines; Indoles; Gliotoxin; Alkyl and Aryl Transferases; Recombinant Proteins; Enzyme Inhibitors; Structure-Activity Relationship; Genes, ras; Farnesyltranstransferase
Subjects: R Medicine > RC Internal medicine > RC0254 Neoplasms. Tumors. Oncology (including Cancer)
Divisions: Faculty of Science and Health
Faculty of Science and Health > Life Sciences, School of
SWORD Depositor: Elements
Depositing User: Elements
Date Deposited: 26 Jun 2017 12:06
Last Modified: 11 Apr 2022 11:04
URI: http://repository.essex.ac.uk/id/eprint/8310

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