Abstract
— 2-Methoxyestradiol (2ME2), a natural metabolite of estradiol which has no estrogenic activity, is a potent antitumor and anti-angiogenic compound, currently undergoing clinical trials for treatment of a variety of cancers. In the last two decades, an ever increasing number of synthetic 2-methoxyestradiol analogues have been reported. Structural changes include A/B/C/D-rings modification, homologation, aromatization, and introduction of various substituents on C-2 position along with substitution of alkyl and ethynyl groups for the 17-hydroxy function. In this review, an attempt has been made to compile the structure-activity relationships of various synthesized 2-methoxyestradiol analogues.
Keywords: — 2-Methoxyestradiol, antiproliferative activity, antimitotic activity, apoptotic activity, antiangiogenesis, anticancer agents, structure-activity relationships, homologation, aromatization, ethynyl groups.
Current Medicinal Chemistry
Title:Synthetic 2-Methoxyestradiol Derivatives: Structure-Activity Relationships
Volume: 19 Issue: 24
Author(s): Jean-Francois Peyrat, Jean-Daniel Brion and Mouad Alami
Affiliation:
Keywords: — 2-Methoxyestradiol, antiproliferative activity, antimitotic activity, apoptotic activity, antiangiogenesis, anticancer agents, structure-activity relationships, homologation, aromatization, ethynyl groups.
Abstract: — 2-Methoxyestradiol (2ME2), a natural metabolite of estradiol which has no estrogenic activity, is a potent antitumor and anti-angiogenic compound, currently undergoing clinical trials for treatment of a variety of cancers. In the last two decades, an ever increasing number of synthetic 2-methoxyestradiol analogues have been reported. Structural changes include A/B/C/D-rings modification, homologation, aromatization, and introduction of various substituents on C-2 position along with substitution of alkyl and ethynyl groups for the 17-hydroxy function. In this review, an attempt has been made to compile the structure-activity relationships of various synthesized 2-methoxyestradiol analogues.
Export Options
About this article
Cite this article as:
Peyrat Jean-Francois, Brion Jean-Daniel and Alami Mouad, Synthetic 2-Methoxyestradiol Derivatives: Structure-Activity Relationships, Current Medicinal Chemistry 2012; 19 (24) . https://dx.doi.org/10.2174/092986712802430072
DOI https://dx.doi.org/10.2174/092986712802430072 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
Call for Papers in Thematic Issues
Advances in Medicinal Chemistry: From Cancer to Chronic Diseases.
The broad spectrum of the issue will provide a comprehensive overview of emerging trends, novel therapeutic interventions, and translational insights that impact modern medicine. The primary focus will be diseases of global concern, including cancer, chronic pain, metabolic disorders, and autoimmune conditions, providing a broad overview of the advancements in ...read more
Approaches to the treatment of chronic inflammation
Chronic inflammation is a hallmark of numerous diseases, significantly impacting global health. Although chronic inflammation is a hot topic, not much has been written about approaches to its treatment. This thematic issue aims to showcase the latest advancements in chronic inflammation treatment and foster discussion on future directions in this ...read more
Cellular and Molecular Mechanisms of Non-Infectious Inflammatory Diseases: Focus on Clinical Implications
The Special Issue covers the results of the studies on cellular and molecular mechanisms of non-infectious inflammatory diseases, in particular, autoimmune rheumatic diseases, atherosclerotic cardiovascular disease and other age-related disorders such as type II diabetes, cancer, neurodegenerative disorders, etc. Review and research articles as well as methodology papers that summarize ...read more
Chalcogen-modified nucleic acid analogues
Chalcogen-modified nucleosides, nucleotides and oligonucleotides have been of great interest to scientific research for many years. The replacement of oxygen in the nucleobase, sugar or phosphate backbone by chalcogen atoms (sulfur, selenium, tellurium) gives these biomolecules unique properties resulting from their altered physical and chemical properties. The continuing interest in ...read more
- 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
- Announcements
Related Articles
-
Alpha-1 Antitrypsin: It’s Role in Health and Disease
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Potential Application of Non-flavonoid Phenolics in Diabetes: Antiinflammatory Effects
Current Medicinal Chemistry Cerebrovascular Complications of Diabetes: Focus on Stroke
Endocrine, Metabolic & Immune Disorders - Drug Targets Treatment of HCV-Related Mixed Cryoglobulinemia
Current Drug Targets Pediatric CKD and Cardivascular Disease
Cardiovascular & Hematological Disorders-Drug Targets Potential Cardio-Protective Agents: A Resveratrol Review (2000-2019)
Current Pharmaceutical Design Anti-Tumor Monoclonal Antibodies in Conjunction with β-Glucans: A Novel Anti- Cancer Immunotherapy
Current Medicinal Chemistry Virus-Associated Vasculitides
Current Immunology Reviews (Discontinued) Perspectives on Medicinal Properties of Mangiferin
Mini-Reviews in Medicinal Chemistry Defining and Regulating Acute Inflammatory Lesion Formation during the Pathogenesis of Multiple Sclerosis and Experimental Autoimmune Encephalomyelitis
CNS & Neurological Disorders - Drug Targets Could Better Phenotyping Small Vessel Disease Provide New Insights into Alzheimer Disease and Improve Clinical Trial Outcomes?
Current Alzheimer Research Pathophysiology of Myocardial Infarction and Acute Management Strategies
Cardiovascular & Hematological Agents in Medicinal Chemistry Resident Kidney Cells and Their Involvement in Glomerulonephritis
Current Drug Targets - Inflammation & Allergy Myeloperoxidase: The Good, the Bad, and the Ugly
Current Immunology Reviews (Discontinued) Pharmacologic Ovarian Preservation in Young Women Undergoing Chemotherapy
Current Medicinal Chemistry Pharmacologic Treatment of Pulmonary Arterial Hypertension
Current Pharmaceutical Design Mechanisms of Corticosteroid Resistance in Severe Asthma and Chronic Obstructive Pulmonary Disease (COPD)
Current Pharmaceutical Design Autoantibodies Among HIV-1 Infected Individuals and the Effect of Anti-Retroviral Therapy (ART) on It
Current HIV Research Regulatory Roles of the Ubiquitin-Proteasome System in Cardiomyocyte Apoptosis
Current Molecular Medicine Effectiveness of Long-Term Macrolide Therapy in Cryptogenic Organising Pneumonia
Current Respiratory Medicine Reviews