Abstract
We report the results of the synthesis and biochemical evaluation of esters of 4-[(aminosulfonyl)oxy]benzoate as potential inhibitors of estrone sulfatase (ES). Modelling the compounds shows that steric interaction between the inhibitor and the active site is a major factor responsible for the weak inhibitory activity observed within the synthesised compounds.
Keywords: Estrone sulfatase, Synthesis, Evaluation, Cycloalkyl esters, Breast cancer, Inhibition
Letters in Drug Design & Discovery
Title: Synthesis and In Vitro Biochemical Evaluation of a Series of Cycloalkyl Esters of 4-Sulfamoylated Benzoic Acid as Inhibitors of Estrone Sulfatase (ES)
Volume: 4 Issue: 6
Author(s): Caroline P. Owen, Chirag K. Patel, Tim Cartledge and Sabbir Ahmed
Affiliation:
Keywords: Estrone sulfatase, Synthesis, Evaluation, Cycloalkyl esters, Breast cancer, Inhibition
Abstract: We report the results of the synthesis and biochemical evaluation of esters of 4-[(aminosulfonyl)oxy]benzoate as potential inhibitors of estrone sulfatase (ES). Modelling the compounds shows that steric interaction between the inhibitor and the active site is a major factor responsible for the weak inhibitory activity observed within the synthesised compounds.
Export Options
About this article
Cite this article as:
Caroline P. Owen , Chirag K. Patel , Tim Cartledge and Sabbir Ahmed , Synthesis and In Vitro Biochemical Evaluation of a Series of Cycloalkyl Esters of 4-Sulfamoylated Benzoic Acid as Inhibitors of Estrone Sulfatase (ES), Letters in Drug Design & Discovery 2007; 4 (6) . https://dx.doi.org/10.2174/157018007781387845
DOI https://dx.doi.org/10.2174/157018007781387845 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
Related Journals
Related Books
- 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
-
Review on Triggered Liposomal Drug Delivery with a Focus on Ultrasound
Current Cancer Drug Targets Regional Anesthesia and Analgesia: Their Role in Postoperative Outcome
Current Topics in Medicinal Chemistry Spectroscopic Characterization of a Pyridine Alkaloid from an Endophytic Strain of the Fusarium incarnatum-equiseti Species Complex
Current Bioactive Compounds Recent Advances in the New Generation Taxane Anticancer Agents
Medicinal Chemistry Dynamic Contrast Enhanced Magnetic Resonance Imaging in Oncology:Theory, Data Acquisition,Analysis, and Examples
Current Medical Imaging Up-Regulation of Gr1+CD11b+ Population in Spleen of Dextran Sulfate Sodium Administered Mice Works to Repair Colitis
Inflammation & Allergy - Drug Targets (Discontinued) Salmonella as Live Trojan Horse for Vaccine Development and Cancer Gene Therapy
Current Gene Therapy Synthesis, Characterization and Cholinesterase Inhibition Studies of New Arylidene Aminothiazolylethanone Derivatives
Medicinal Chemistry Predicting Toxicity: Biomarkers and the Value of the Patient's Opinion
Current Pharmaceutical Design An Updated Review of Natural Products Intended to Prevent or Treat Oral Mucositis in Patients Undergoing Radio-Chemotherapy
Current Pharmaceutical Biotechnology A Discriminative Feature Extraction Approach for Tumor Classification Using Gene Expression Data
Current Bioinformatics Resistance of Cancer Cells to Targeted Therapies Through the Activation of Compensating Signaling Loops
Current Signal Transduction Therapy ADAM Metalloproteinases as Potential Drug Targets
Current Medicinal Chemistry Autofluorescence of Breast Cancer Proteins
Current Metabolomics Rasburicase: A New Approach for Preventing and/or Treating Tumor Lysis Syndrome
Current Pharmaceutical Design Nutritional and Therapeutic Potential of Garlic and Onion (Allium sp.)
Current Nutrition & Food Science A Potent Inhibitor of Steroid Sulfatase (EM-1913) Blocks Tumor Growth in Nude Mice (MCF-7 Xenograft)
Current Enzyme Inhibition Targeting Mevalonate Pathway in Cancer Treatment: Repurposing of Statins
Recent Patents on Anti-Cancer Drug Discovery Thromboprophylaxis in Medical Patients: An Update
Vascular Disease Prevention (Discontinued) PET Imaging of Multidrug Resistance in Tumors Using 18F-Fluoropaclitaxel
Current Topics in Medicinal Chemistry