Abstract
The endogenous steroid 2-methoxyestradiol (2-ME) is a metabolite of 17-estradiol and its biosynthesis is well established. Moreover, 2-ME is also biosynthesized from estrone. For several years, 2-ME was perceived as an inactive metabolite devoid of any interesting biological activities. Since the late 1980s, a number of biological and pharmacological studies have revealed that 2-ME possesses interesting anti-cancer effects without any undesirable estrogen activity. In particular, the anti-vascular effects and anti-angiogenic activities that 2-ME exhibit, are of great interest and importance, in view of the development of new anti-cancer drugs based on 2-ME. Several clinical trial development programs have been initiated using the steroid 2-ME. In addition, based on the many pharmacological activities reported for 2-ME, but also due to the general interest in total and semi-synthesis of endogenous steroids, several research groups working with organic synthesis have prepared this steroid. Herein, the anti-cancer effects, the results from the clinical trial development programs and the synthetic studies towards 2-ME, are reviewed.
Keywords: Steroid, 2-methoxyestradiol, anti-cancer effects, anti-vascular effects, anti-angiogenic activities, tubulin inhibition, clinical trials, total synthesis, regioselectivity.
Current Pharmaceutical Design
Title:Synthesis and Pharmacological Effects of the Anti-Cancer Agent 2-Methoxyestradiol
Volume: 21 Issue: 38
Author(s): Eirik Johansson Solum, Oyvind W. Akselsen, Anders Vik and Trond Vidar Hansen
Affiliation:
Keywords: Steroid, 2-methoxyestradiol, anti-cancer effects, anti-vascular effects, anti-angiogenic activities, tubulin inhibition, clinical trials, total synthesis, regioselectivity.
Abstract: The endogenous steroid 2-methoxyestradiol (2-ME) is a metabolite of 17-estradiol and its biosynthesis is well established. Moreover, 2-ME is also biosynthesized from estrone. For several years, 2-ME was perceived as an inactive metabolite devoid of any interesting biological activities. Since the late 1980s, a number of biological and pharmacological studies have revealed that 2-ME possesses interesting anti-cancer effects without any undesirable estrogen activity. In particular, the anti-vascular effects and anti-angiogenic activities that 2-ME exhibit, are of great interest and importance, in view of the development of new anti-cancer drugs based on 2-ME. Several clinical trial development programs have been initiated using the steroid 2-ME. In addition, based on the many pharmacological activities reported for 2-ME, but also due to the general interest in total and semi-synthesis of endogenous steroids, several research groups working with organic synthesis have prepared this steroid. Herein, the anti-cancer effects, the results from the clinical trial development programs and the synthetic studies towards 2-ME, are reviewed.
Export Options
About this article
Cite this article as:
Solum Johansson Eirik, Akselsen W. Oyvind, Vik Anders and Hansen Vidar Trond, Synthesis and Pharmacological Effects of the Anti-Cancer Agent 2-Methoxyestradiol, Current Pharmaceutical Design 2015; 21 (38) . https://dx.doi.org/10.2174/1381612821666151002112511
DOI https://dx.doi.org/10.2174/1381612821666151002112511 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Blood-based biomarkers in large-scale screening for neurodegenerative diseases
Disease biomarkers are necessary tools that can be employ in several clinical context of use (COU), ranging from the (early) diagnosis, prognosis, prediction, to monitor of disease state and/or drug efficacy. Regarding neurodegenerative diseases, in particular Alzheimer’s disease (AD), a battery of well-validated biomarkers are available, such as cerebrospinal fluid ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Diabetes mellitus: advances in diagnosis and treatment driving by precision medicine
Diabetes mellitus (DM) is a chronic degenerative metabolic disease with ever increasing prevalence worldwide which is now an epidemic disease affecting 500 million people worldwide. Insufficient insulin secretion from pancreatic β cells unable to maintain blood glucose homeostasis is the main feature of this disease. Multifactorial and complex nature of ...read more
![](/images/wayfinder.jpg)
- 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
-
Berberine Exhibits Antitumor Effects in Human Ovarian Cancer Cells
Anti-Cancer Agents in Medicinal Chemistry BRCA1-Associated Triple-Negative Breast Cancer and Potential Treatment for Ruthenium-Based Compounds
Current Cancer Drug Targets Aspirin as a Chemoprevention Agent for Colorectal Cancer
Current Drug Metabolism Biocompatible Magnetic Hollow Silica Microspheres for Drug Delivery
Current Organic Chemistry Development for Anticancer Therapy: Small-Molecule Inhibitors Targeting Protein Kinase B
Mini-Reviews in Medicinal Chemistry Pieces of the Complex Puzzle of Cancer Cell Energy Metabolism: An Overview of Energy Metabolism and Alternatives for Targeted Cancer Therapy
Current Medicinal Chemistry Evaluation of Anti-cancer Activity of Stilbene and Methoxydibenzo[b,f] oxepin Derivatives
Current Cancer Drug Targets Gut Microbiota and Alcoholic Liver Disease
Reviews on Recent Clinical Trials Regulation of Cell Growth by Estrogen Signaling and Potential Targets in Thyroid Cancer
Current Cancer Drug Targets Applications of FDG-PET/CT in Assessment of Vascular Infection and Inflammation
Current Molecular Imaging (Discontinued) Liver Transporters in Hepatic Drug Disposition: An Update
Current Drug Metabolism Steroid Receptor Ligands for Breast Cancer Targeting: An Insight into Their Potential Role As Pet Imaging Agents
Current Medicinal Chemistry Current Evidence from Phase III Clinical Trials of Selenium Supplementation in Critically Ill Patients: Why Should We Bother?
Mini-Reviews in Medicinal Chemistry Colony-Stimulating Factor-1 Receptor Inhibitors for the Treatment of Cancer and Inflammatory Disease
Current Topics in Medicinal Chemistry Editorial: [Recent Advances in Mammography]
Recent Patents on Medical Imaging Editorial
Current Medical Imaging Mesenchymal Stem Cells Derived from Wharton's Jelly of the Umbilical Cord: Biological Properties and Emerging Clinical Applications
Current Stem Cell Research & Therapy Basic Approaches in Therapy of Multiple Sclerosis (MS) and Related Diseases: Current Achievement and Prospective
Central Nervous System Agents in Medicinal Chemistry Sporadic Porphyria in a Patient with Stage II Melanoma Treated with Interferon α
Current Drug Safety SYNTHESIS AND APPLICATIONS OF Fe3O4/SiO2 CORE-SHELL MATERIALS
Current Pharmaceutical Design