Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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An Approach Towards the Quantitative Structure-Activity Relationships for Sulfamate-Based Estrone Sulfatase Inhibitors

Author(s): Rajeshwar P. Verma.

Abstract:

Estrone sulfatase (ES) is a membrane-bound enzyme that is responsible for maintaining high levels of estrogens in breast cancer cells. This may be due to the conversion of estrone-sulfate into estrone by estronesulfatase, which acts as a pool of potentially available estrogens. There is now abundant evidence that estrogens have a pivotal role in the growth and development of hormone-dependent breast cancer. Thus, inhibitors of ES should have considerable therapeutic potential for the treatment of hormone-dependent breast cancer. Recently, a large number of sulfamate-based steroidal and non-steroidal ES inhibitors have been developed. The sulfamate moiety is believed to be involved in the irreversible inhibition of ES. In the present paper, we have undertaken quantitative structure-activity relationships for different series of non-steroidal sulfamate-based compounds in order to understand the chemical-biological interactions governing their inhibitory potency against ES. QSAR results have shown that the inhibitory potency against ES for these nonsteroidal sulfamate-based compounds is largely dependent on their hydrophobicity and molar refractivity.

Keywords: breast cancer, estrone sulfatase inhibitors, hydrophobicity, molar refractivity, non-steroidal sulfamates, structureactivity relationships

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Article Details

VOLUME: 2
ISSUE: 3
Year: 2005
Page: [205 - 218]
Pages: 14
DOI: 10.2174/1570180053765093
Price: $58