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. DOI https://doi.org/10.1016/j.bmcl.2003.08.022
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. DOI https://doi.org/10.1016/j.bmcl.2003.08.022
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. DOI https://doi.org/10.1016/j.bmcl.2003.08.022
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: | Unnamed user with email elements@essex.ac.uk |
| Depositing User: | Unnamed user with email elements@essex.ac.uk |
| Date Deposited: | 26 Jun 2017 12:06 |
| Last Modified: | 30 Oct 2024 19:21 |
| URI: | http://repository.essex.ac.uk/id/eprint/8310 |