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), 209-215.

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Description/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.

Item Type: Article
ISSNs: 0266-9536 (print)
Related URLs:
Subjects: R Medicine > RC Internal medicine > RC0254 Neoplasms. Tumors. Oncology (including Cancer)
Divisions: University Structure - Pre August 2011 > School of Medicine > Cancer Sciences
ePrint ID: 26666
Date Deposited: 24 Apr 2006
Last Modified: 27 Mar 2014 18:15
URI: http://eprints.soton.ac.uk/id/eprint/26666

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