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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Molecular Modelling, Design, Synthesis and Biochemical Evaluation of a Range of Non-Steroidal Thiosemicarbazone-Based Inhibitors of Estrone Sulfatase (ES) - A Potential Insight into the Action of a Range of Allosteric Inhibitors of ES

Author(s): Amit Kumar, Sukriti Singh, Balkrishna Bhamare, Kruti Shah, Pallav S. Shah and Sabbir Ahmed

Volume 8, Issue 9, 2011

Page: [889 - 896] Pages: 8

DOI: 10.2174/157018011797200821

Price: $65

Abstract

Results of the modelling of thiosemicarbazone-based inhibitors of ES suggest that these compounds interact with the calcium ion whilst undergoing hydrogen bonding interaction with the active site - the extent of H-bonding determining the overall inhibitory activity. Novel inhibitors were designed, synthesised and evaluated and found to possess potent inhibitory activity.

Keywords: Allosteric inhibitors, Breast cancer, Estrone sulfatase, Estrone sulfatase, Non-steroidal inhibitors, Thiosemicarbazones, estrogens, coumarin-based compounds, inhibitory activity, phenacyl bromides, sulfamate-based inhibitors, cancer, Elkay, diaryl ketoximes, American Type Culture Collection (ATCC), Rota rod method


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