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Inhibition of superoxide dismutase by 2-methoxyoestradiol analogues and oestrogen derivatives - structure-activity relationships

Wood, L., Leese, M.R., Leblond, B., Woo, L.W., Ganeshapillai, D., Purohit, A., Reed, M.J., Potter, B.V. and Packham, G. (2001) Inhibition of superoxide dismutase by 2-methoxyoestradiol analogues and oestrogen derivatives - structure-activity relationships Anti-Cancer Drug Design, 16, (4-5), pp. 209-215.

Record type: Article

Abstract

Superoxide dismutases catalyse the dismutation of highly reactive superoxide ions to produce hydrogen peroxide and several lines of evidence suggest that these enzymes play important roles in the development and response to treatment of human cancers. For example, Mn-containing superoxide dismutase is frequently overexpressed in various cancer types and can contribute to resistance to apoptosis. 2-Methoxyoestradiol is a naturally occurring metabolic product of 17bgr-oestradiol that inhibits tubulin polymerization and possesses growth inhibitory and cytotoxic activity in vitro and in vivo. More recently 2-methoxyoestradiol has also been shown to inhibit superoxide dismutase (SOD) in a tetrazolium salt based enzyme assay, suggesting that oestrogen derivatives might be useful starting points for the development of effective, non-toxic enzyme inhibitors. Here we have tested the SOD inhibiting activity of a range of oestrogen derivatives to determine structural features important for enzyme inhibition.

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Published date: 2001

Identifiers

Local EPrints ID: 26666
URI: http://eprints.soton.ac.uk/id/eprint/26666
ISSN: 0266-9536
PURE UUID: f0ebe4bf-8eab-4dae-b8ef-deaff145a6b3

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Date deposited: 24 Apr 2006
Last modified: 17 Jul 2017 16:06

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Contributors

Author: L. Wood
Author: M.R. Leese
Author: B. Leblond
Author: L.W. Woo
Author: D. Ganeshapillai
Author: A. Purohit
Author: M.J. Reed
Author: B.V. Potter
Author: G. Packham

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