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
-
Structural Modifications of Matrine-Type Alkaloids
Mini-Reviews in Medicinal Chemistry Targeting Tumour Metastasis: The Emerging Role of Nanotechnology
Current Medicinal Chemistry Signaling Through Rho GTPase Pathway as Viable Drug Target
Current Medicinal Chemistry History and Milestones of Mouse Models of Autoimmune Diseases
Current Pharmaceutical Design The Insulin-Like Growth Factor (IGF) Signaling Pathway: Strategies for Successful Therapeutic Tasks in Cancer Treatment
Current Cancer Therapy Reviews Micro-RNA in Disease and Gene Therapy
Current Drug Discovery Technologies Mechanisms Involved in Metformin Action in the Treatment of Polycystic Ovary Syndrome
Current Pharmaceutical Design Synthesis, Cytotoxic and Heparanase Inhibition Studies of 5-oxo-1-arylpyrrolidine-3- carboxamides of Hydrazides and 4-amino-5-aryl-4H-1,2,4-triazole-3-thiol
Current Organic Synthesis Biosafety of Recombinant Adeno-associated Virus Vectors
Current Gene Therapy Targeting Stem Cells-Clinical Implications for Cancer Therapy
Current Stem Cell Research & Therapy Targeting the Ubiquitin E1 as a Novel Anti-Cancer Strategy
Current Pharmaceutical Design Synthesis and in vitro Cytotoxicity Studies of Certain Novel Heterocycles Derived from Bis 1, 2, 4-Triazoles and their DNA Damage Studies
Medicinal Chemistry Ras Dimer Formation as a New Signaling Mechanism and Potential Cancer Therapeutic Target
Mini-Reviews in Medicinal Chemistry Synthesis and Evaluation of Certain Symmetrical Schiff Bases as Inhibitors of MDA-MB-241 Human Breast Cancer Cell Proliferation
Letters in Drug Design & Discovery Plant Polyphenols and Tumors: From Mechanisms to Therapies, Prevention, and Protection Against Toxicity of Anti-Cancer Treatments
Current Medicinal Chemistry Sphingosine Kinases Signalling in Carcinogenesis
Mini-Reviews in Medicinal Chemistry The Gut-Brain Axis, Including the Microbiome, Leaky Gut and Bacterial Translocation: Mechanisms and Pathophysiological Role in Alzheimer’s Disease
Current Pharmaceutical Design The Genus Glycosmis [Rutaceae]: A Comprehensive Review on its Phytochemical and Pharmacological Perspectives
The Natural Products Journal Gallium-68: A New Trend in PET Radiopharmacy
Current Radiopharmaceuticals Focus on the Multimodal Role of Biomarkers in Breast Cancer
Current Pharmaceutical Design