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, Sabbir Ahmed.

Journal Name: Letters in Drug Design & Discovery

Volume 8 , Issue 9 , 2011

Become EABM
Become Reviewer

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

Rights & PermissionsPrintExport Cite as

Article Details

VOLUME: 8
ISSUE: 9
Year: 2011
Page: [889 - 896]
Pages: 8
DOI: 10.2174/157018011797200821
Price: $65

Article Metrics

PDF: 1