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

Title: 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

Volume: 8 Issue: 9

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

Affiliation:

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

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.

Cite this article as:

Kumar Amit, Singh Sukriti, Bhamare Balkrishna, Shah Kruti, S. Shah Pallav and Ahmed Sabbir, 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, Letters in Drug Design & Discovery 2011; 8 (9) . https://dx.doi.org/10.2174/157018011797200821