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
Letters in Drug Design & Discovery
Title: An Approach Towards the Quantitative Structure-Activity Relationships for Sulfamate-Based Estrone Sulfatase Inhibitors
Volume: 2 Issue: 3
Author(s): Rajeshwar P. Verma
Affiliation:
Keywords: breast cancer, estrone sulfatase inhibitors, hydrophobicity, molar refractivity, non-steroidal sulfamates, structureactivity relationships
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.
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Cite this article as:
Verma P. Rajeshwar, An Approach Towards the Quantitative Structure-Activity Relationships for Sulfamate-Based Estrone Sulfatase Inhibitors, Letters in Drug Design & Discovery 2005; 2 (3) . https://dx.doi.org/10.2174/1570180053765093
DOI https://dx.doi.org/10.2174/1570180053765093 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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