Abstract
Sulfonate derivatives of estrone (E1) were designed and synthesized as potential reversible inhibitors of E1 sulfatase (ES). The results of the biochemical evaluation show the compounds to be weak inhibitors in comparison to the irreversible inhibitor E1-3-O-sulfamate, however, two compounds were found to possess good inhibitory activity.
Keywords: Breast cancer, Estrone sulfatase, Reversible inhibition, Substrate mimic, Sulfonated derivative.
Letters in Drug Design & Discovery
Title:Synthesis, Biological Evaluation and the Rationalisation of the Inhibitory Activity of a Range of Sulfonate Derivatives of Estrone (E1) in the Design of Reversible Inhibitors of Estrone Sulfatase (ES)
Volume: 11 Issue: 8
Author(s): Mohsen Akbarzadeh, Timothy Cartledge and Sabbir Ahmed
Affiliation:
Keywords: Breast cancer, Estrone sulfatase, Reversible inhibition, Substrate mimic, Sulfonated derivative.
Abstract: Sulfonate derivatives of estrone (E1) were designed and synthesized as potential reversible inhibitors of E1 sulfatase (ES). The results of the biochemical evaluation show the compounds to be weak inhibitors in comparison to the irreversible inhibitor E1-3-O-sulfamate, however, two compounds were found to possess good inhibitory activity.
Export Options
About this article
Cite this article as:
Akbarzadeh Mohsen, Cartledge Timothy and Ahmed Sabbir, Synthesis, Biological Evaluation and the Rationalisation of the Inhibitory Activity of a Range of Sulfonate Derivatives of Estrone (E1) in the Design of Reversible Inhibitors of Estrone Sulfatase (ES), Letters in Drug Design & Discovery 2014; 11 (8) . https://dx.doi.org/10.2174/1570180811666140226235116
DOI https://dx.doi.org/10.2174/1570180811666140226235116 |
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
-
Diallyl Disulfide Inhibits Breast Cancer Stem Cell Progression and Glucose Metabolism by Targeting CD44/PKM2/AMPK Signaling
Current Cancer Drug Targets Anti-Angiogenic Agents and Cancer: Current Insights and Future Perspectives
Recent Patents on Anti-Cancer Drug Discovery HTLV-1-Associated Myelopathy/Tropical Spastic Paraparesis (HAM/TSP) Inflammatory Network
Inflammation & Allergy - Drug Targets (Discontinued) Advances of Paclitaxel Formulations Based on Nanosystem Delivery Technology
Mini-Reviews in Medicinal Chemistry Role of COL4A1 in Basement-Membrane Integrity and Cerebral Small-Vessel Disease. The COL4A1 Stroke Syndrome
Current Medicinal Chemistry Prevention of VP-16 Resistance by a Disiloxane, SILA409: Effects of SILA409 on the Expression of GRP78 in NCI-H446 Human Small Cell Lung Cancer Cells
Letters in Drug Design & Discovery Cancer Therapeutics: Emerging Targets and Trends
Current Cancer Therapy Reviews Other Future Targeting Therapy Beyond TNF-α Inhibitor in Patients with Spondyloarthropathy
Current Rheumatology Reviews Drug Delivery Systems for Brain Tumor Therapy
Current Pharmaceutical Design Nucleosides with Modified Sugar Ring: Synthesis and Biological Activities
Current Organic Chemistry N-3 (Omega-3) Polyunsaturated Fatty Acids in the Pathophysiology and Treatment of Depression: Pre-Clinical Evidence
CNS & Neurological Disorders - Drug Targets Dry Age-Related Macular Degeneration: Recent Progress of Therapeutic approaches
Current Molecular Pharmacology Fabry Disease Cardiomyopathy: from Genes to Clinical Manifestations
Current Pharmaceutical Biotechnology Recent Progress of Src Family Kinase Inhibitors as Anticancer Agents
Mini-Reviews in Medicinal Chemistry Alpha1-Antitrypsin Deficiency: Transition of Care for the Child With AAT Deficiency into Adulthood
Current Pediatric Reviews Multitargeted Molecular Docking Study of Natural-Derived Alkaloids on Breast Cancer Pathway Components
Current Computer-Aided Drug Design Synthesis and Antitumor Activity of Novel 4-Chloro-3-Arylmaleimide Derivatives
Letters in Drug Design & Discovery Overview of SLC22A and SLCO Families of Drug Uptake Transporters in the Context of Cancer Treatments
Current Drug Metabolism Structure-Function Relationship of Vpr: Biological Implications
Current HIV Research Hepato and Cardiotoxicity of Chemotherapeutic Treatment Evaluated by Means of Small Animal Imaging
Anti-Cancer Agents in Medicinal Chemistry