Abstract
We report the results of our study into a series of 3,5-dibrominated derivatives of esters of 4- [(aminosulfonyl)oxy]benzoate as potential inhibitors of estrone sulfatase (ES). The results suggest that the compounds are weak inhibitors as a result of the incorporation of the bromine atoms which reduce the stability of the compound.
Keywords: Estrone sulfatase, Inhibition, Breast cancer pKa, Dibrominated, Benzoic acid esters
Letters in Drug Design & Discovery
Title: Synthesis and In Vitro Biochemical Evaluation of a Series of Compounds as Potential Inhibitors of Estrone Sulfatase (ES) and the Role of pKa in both the Synthesis and the Inhibitory Activity of the Potential Inhibitors
Volume: 4 Issue: 6
Author(s): Caroline P. Owen, Mijal Patel, Chirag K Patel, Tim Cartledge and Sabbir Ahmed
Affiliation:
Keywords: Estrone sulfatase, Inhibition, Breast cancer pKa, Dibrominated, Benzoic acid esters
Abstract: We report the results of our study into a series of 3,5-dibrominated derivatives of esters of 4- [(aminosulfonyl)oxy]benzoate as potential inhibitors of estrone sulfatase (ES). The results suggest that the compounds are weak inhibitors as a result of the incorporation of the bromine atoms which reduce the stability of the compound.
Export Options
About this article
Cite this article as:
Caroline P. Owen , Mijal Patel , Chirag K Patel , Tim Cartledge and Sabbir Ahmed , Synthesis and In Vitro Biochemical Evaluation of a Series of Compounds as Potential Inhibitors of Estrone Sulfatase (ES) and the Role of pKa in both the Synthesis and the Inhibitory Activity of the Potential Inhibitors, Letters in Drug Design & Discovery 2007; 4 (6) . https://dx.doi.org/10.2174/157018007781387773
DOI https://dx.doi.org/10.2174/157018007781387773 |
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
-
Annexins in the Central Nervous System: Are they Neuroprotective or Proapoptotic Agents?
Medicinal Chemistry Reviews - Online (Discontinued) Recent Developments in Targeting Breast Cancer Stem Cells
Recent Patents on Regenerative Medicine Beneficial Effects of Herbs, Spices and Medicinal Plants on the Metabolic Syndrome, Brain and Cognitive Function
Central Nervous System Agents in Medicinal Chemistry Effects of Natural Products on Mcl-1 Expression and Function
Current Medicinal Chemistry An Update on JAK Inhibitors
Current Medicinal Chemistry Provoking Neuroprotection by Peroxynitrite
Current Pharmaceutical Design Mini-Review: Bmx Kinase Inhibitors for Cancer Therapy
Recent Patents on Anti-Cancer Drug Discovery Novel Anti-Cancer Strategy in Bone Tumors by Targeting Molecular and Cellular Modulators of Bone Resorption
Recent Patents on Anti-Cancer Drug Discovery Detection of Melatonin Production from the Intestinal Epithelium Using Electrochemical Methods
Current Pharmaceutical Design Pharmacokinetic and Toxicological Characteristics of Tripterigium Glycosides and Their Derivatives
Current Drug Metabolism Applications of Lipid-based Nanocarriers for Parenteral Drug Delivery
Current Medicinal Chemistry Development of Patents and Clinical Trials on Regenerative Therapy: Gene Therapy
Recent Patents on Regenerative Medicine Estrogen and Female Lower Urinary Tract Dysfunction
Current Women`s Health Reviews Pyrano[3,2-c]quinoline Derivatives as New Class of α-glucosidase Inhibitors to Treat Type 2 Diabetes: Synthesis, in vitro Biological Evaluation and Kinetic Study
Medicinal Chemistry JAK Inhibitors: Pharmacology and Clinical Activity in Chronic Myeloprolipherative Neoplasms
Current Medicinal Chemistry Role of FoxM1 in the Progression and Epithelial to Mesenchymal Transition of Gastrointestinal Cancer
Recent Patents on Anti-Cancer Drug Discovery Use of Anticancer Platinum Compounds in Combination Therapies and Challenges in Drug Delivery
Current Medicinal Chemistry Application of Mesenchymal Stem Cells in Melanoma: A Potential Therapeutic Strategy for Delivery of Targeted Agents
Current Medicinal Chemistry The Importance of c-Kit and PDGF Receptors as Potential Targets for Molecular Therapy in Breast Cancer
Current Medicinal Chemistry Genetics and Ulcerative Colitis: What are the Clinical Implications?
Current Drug Targets