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
Pallav S. Shah,
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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