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
Letters in Drug Design & Discovery
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.
Export Options
About this article
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
DOI https://dx.doi.org/10.2174/157018011797200821 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Phytoestrogens in Postmenopause: The State of the Art from a Chemical, Pharmacological and Regulatory Perspective
Current Medicinal Chemistry The Potential Role of Claudins in Regulation of Metastasis and Development of Drug Resistance in Breast Cancer
Clinical Cancer Drugs Antiproliferative and Antioxidant Potential of Leaf and Leaf Derived Callus Extracts of Aerva lanata (L.) Juss. Ex Schult. Against Human Breast Cancer (MCF-7) Cell Lines
The Natural Products Journal Cancer Biomarker Discovery for Precision Medicine: New Progress
Current Medicinal Chemistry Importance of Aquaporins in the Physiopathology of Brain Edema
Current Pharmaceutical Design Biological Activity of Carotenoids: Its Implications in Cancer Risk and Prevention
Current Pharmaceutical Biotechnology Alternative Polyadenylation and Its Impact on Cellular Processes
MicroRNA Soothing the Inflamed Brain: Effect of Non-Steroidal Anti-Inflammatory Drugs on Alzheimers Disease Pathology
CNS & Neurological Disorders - Drug Targets Synthesis and Preliminary Biological Evaluation of New Heterocyclic Carboxamide Models
Letters in Drug Design & Discovery PLGA Nanoparticles for Nose to Brain Delivery of Clonazepam: Formulation, Optimization by 32 Factorial Design, In Vitro and In Vivo Evaluation
Current Drug Delivery A Rationale for the Use of Proton Pump Inhibitors as Antineoplastic Agents
Current Pharmaceutical Design Antibody-Based Imaging of HER-2: Moving into the Clinic
Current Molecular Medicine Bio-analytical Identification of Key Genes that Could Contribute to the Progression and Metastasis of Osteosarcoma
Current Bioinformatics The Potential of Peroxisome Proliferator-Activated Receptor γ (PPARγ) Ligands in the Treatment of Hematological Malignancies
Mini-Reviews in Medicinal Chemistry Patent Selections
Recent Patents on DNA & Gene Sequences Strategies Targeting DNA Topoisomerase I in Cancer Chemotherapy: Camptothecins, Nanocarriers for Camptothecins, Organic Non-Camptothecin Compounds and Metal Complexes
Current Drug Targets Nuclear Long Non-Coding RNAs as Epigenetic Regulators in Cancer
Current Medicinal Chemistry The Use of Lentinan for Treating Gastric Cancer
Anti-Cancer Agents in Medicinal Chemistry EphA2-Dependent Molecular Targeting Therapy for Malignant Tumors
Current Cancer Drug Targets Sympathetic Nervous System Dysfunction in Multiple Sclerosis, Linking Neurodegeneration to a Reduced Response to Therapy
Current Pharmaceutical Design