Abstract
Epothilones are natural compounds isolated from a myxobacterium at the beginning of the 1990s, and showed a remarkable anti-neoplastic activity. They act through the same mechanism of action of paclitaxel, by stabilizing microtubules and inducing apoptosis. Although, their chemical structure, simpler than taxanes, makes them more suitable for derivatization. Their interesting pharmacokinetic and bioavailabilty profiles, and the activity against paclitaxel-resistant cell lines make them interesting therapeutic agents. Here a brief historical perspective of epothilones is presented, since their isolation, the identification of their mechanism of action and activity, to the recent clinical trials.
Keywords: Cancer, Drug design, MDR, Microtubules MSAA, Pharmacophore, SAR, Tubulin.
Graphical Abstract
Current Topics in Medicinal Chemistry
Title:Epothilones: From Discovery to Clinical Trials
Volume: 14 Issue: 20
Author(s): Stefano Forli
Affiliation:
Keywords: Cancer, Drug design, MDR, Microtubules MSAA, Pharmacophore, SAR, Tubulin.
Abstract: Epothilones are natural compounds isolated from a myxobacterium at the beginning of the 1990s, and showed a remarkable anti-neoplastic activity. They act through the same mechanism of action of paclitaxel, by stabilizing microtubules and inducing apoptosis. Although, their chemical structure, simpler than taxanes, makes them more suitable for derivatization. Their interesting pharmacokinetic and bioavailabilty profiles, and the activity against paclitaxel-resistant cell lines make them interesting therapeutic agents. Here a brief historical perspective of epothilones is presented, since their isolation, the identification of their mechanism of action and activity, to the recent clinical trials.
Export Options
About this article
Cite this article as:
Forli Stefano, Epothilones: From Discovery to Clinical Trials, Current Topics in Medicinal Chemistry 2014; 14 (20) . https://dx.doi.org/10.2174/1568026614666141130095855
DOI https://dx.doi.org/10.2174/1568026614666141130095855 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Medicinal Chemistry Advancement in Life-Threatening Diseases
The current issue will highlight concise reports that specify ground-breaking insights, including the novel discovery of drug targets and their action mechanism or drugs of novel classes. These are projected to encourage medicinal chemistry future efforts to address the most challenging medical needs. The current issue highlights further efforts to ...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
-
Small Molecules with EGFR-TK Inhibitor Activity
Current Drug Targets Editorial (Thematic Issue: Metabolic Disorders, Drug Development, Drug Design and Biomarkers)
Current Pharmaceutical Design Synthesis of 2-substituted Furo[3,2-b]pyridines Under Pd/C-Cu Catalysis Assisted by Ultrasound: Their Evaluation as Potential Cytotoxic Agents
Anti-Cancer Agents in Medicinal Chemistry Retinol-Binding Protein 4 and New Adipocytokines in Nonalcoholic Fatty Liver Disease
Current Pharmaceutical Design Drug Delivery Systems and Combination Therapy by Using Vinca Alkaloids
Current Topics in Medicinal Chemistry Synthesis, Antibacterial Activity, Interaction with Nucleobase and Molecular Docking Studies of 4-Formylbenzoic Acid Based Thiazoles
Medicinal Chemistry Targeting Cytokines, Chemokines and Adhesion Molecules in Rheumatoid Arthritis
Current Rheumatology Reviews Differential Gene Expression of BRCA1, ERBB2 and TP53 Biomarkers between Human Breast Tissue and Peripheral Blood Samples of Breast Cancer Patients
Anti-Cancer Agents in Medicinal Chemistry Alternate Strategies of Hsp90 Modulation for the Treatment of Cancer and Other Diseases
Current Topics in Medicinal Chemistry Targeting the Human Epidermal Growth Factor Receptor 2 (HER2) in the Treatment of Breast Cancer: Recent Advances and Future Directions
Reviews on Recent Clinical Trials Dendritic Cell Vaccine and Cancer Treatment: New Patents
Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (Discontinued) Apoptotic Potency of Angiostatic Compounds in the Treatment of Cancer
Current Pharmaceutical Biotechnology Human Apurinic/Apyrimidinic Endonuclease (APE1): An Emerging Anti-Cancer Biomarker
Recent Patents on Biomarkers Localised Delivery of Therapeutic Agents to CNS Malignancies: Old and New Approaches
Current Pharmaceutical Biotechnology Evaluation of Changes in the Expression Profile of mRNA and Proteinencoding Adiponectin in Ishikawa Cell Line under the Influence of Cisplatin – Preliminary Report
Current Pharmaceutical Biotechnology Carotid Artery Atherosclerosis: What is the Evidence for Drug Action?
Current Pharmaceutical Design Ribonucleases, Nucleases and Antiangiogenins in Antiproliferative Activities
Current Signal Transduction Therapy Role of Inflammatory Cells and Toll-Like Receptors in Atherosclerosis
Current Vascular Pharmacology Cytotoxic Constituents from the Bark of Erythrina poeppigiana Against the MCF-7 Breast Cancer Cell Lines
The Natural Products Journal The Non-Canonical IκB Kinases IKKε and TBK1 as Potential Targets for the Development of Novel Therapeutic Drugs
Current Molecular Medicine