Abstract
Paclitaxel belongs to the most successful anticancer drugs developed and utilised during the past two decades. Nevertheless, the development of resistance of tumor cells and severe side effects in the patients require further improvement of the drug. In this review, we provide a detailed overview of the state-of-the-art in the medicinal chemistry of paclitaxel and its analogues. A number of strategies have been explored to obtain sufficient amounts of paclitaxel for clinical use from natural resources. Semi-synthesis from its precursor, 10-deacetylbaccatin III, which can be extracted from Taxus leavesturned out as the most appropriate method for commercial production. So far, many paclitaxel derivatives have been synthesized, and their effect on microtubules stabilization and cytotoxicity were investigated in terms of structure-activity relationships (SAR). One of them, docetaxel, was approved as a more potent anticancer agent than paclitaxel towards a variety of tumor types. This review summarizes current possibilities to harvest sufficient amount of drugs from natural sources, including the production of taxanes in bioreactors and synthetic approaches for paclitaxel and its analogues, their mechanism of action and structure-activity relationships. In addition, future developments and perspectives for this class of compounds are outlined.
Keywords: Paclitaxel, Docetaxel, Taxane, Anti-cancer, Mechanism, SAR, Bioreactor, Taxus
Current Medicinal Chemistry
Title: Medicinal Chemistry of Paclitaxel and its Analogues
Volume: 16 Issue: 30
Author(s): Y. Fu, S. Li, Y. Zu, G. Yang, Z. Yang, M. Luo, S. Jiang, M. Wink and T. Efferth
Affiliation:
Keywords: Paclitaxel, Docetaxel, Taxane, Anti-cancer, Mechanism, SAR, Bioreactor, Taxus
Abstract: Paclitaxel belongs to the most successful anticancer drugs developed and utilised during the past two decades. Nevertheless, the development of resistance of tumor cells and severe side effects in the patients require further improvement of the drug. In this review, we provide a detailed overview of the state-of-the-art in the medicinal chemistry of paclitaxel and its analogues. A number of strategies have been explored to obtain sufficient amounts of paclitaxel for clinical use from natural resources. Semi-synthesis from its precursor, 10-deacetylbaccatin III, which can be extracted from Taxus leavesturned out as the most appropriate method for commercial production. So far, many paclitaxel derivatives have been synthesized, and their effect on microtubules stabilization and cytotoxicity were investigated in terms of structure-activity relationships (SAR). One of them, docetaxel, was approved as a more potent anticancer agent than paclitaxel towards a variety of tumor types. This review summarizes current possibilities to harvest sufficient amount of drugs from natural sources, including the production of taxanes in bioreactors and synthetic approaches for paclitaxel and its analogues, their mechanism of action and structure-activity relationships. In addition, future developments and perspectives for this class of compounds are outlined.
Export Options
About this article
Cite this article as:
Fu Y., Li S., Zu Y., Yang G., Yang Z., Luo M., Jiang S., Wink M. and Efferth T., Medicinal Chemistry of Paclitaxel and its Analogues, Current Medicinal Chemistry 2009; 16 (30) . https://dx.doi.org/10.2174/092986709789352277
DOI https://dx.doi.org/10.2174/092986709789352277 |
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
-
Antioxidant and Antimicrobial Activities of Cinnamic Acid Derivatives
Mini-Reviews in Medicinal Chemistry Multiscale Mapping of AIDS in U.S. Countries vs Anti-HIV Drugs Activity with Complex Networks and Information Indices
Current Bioinformatics New Approaches in Data Integration for Systems Chemical Biology
Current Topics in Medicinal Chemistry Black Fungus: An Alarming Infection During Novel Coronavirus: A Review
Anti-Infective Agents Targeting <i>Malassezia</i> species for Novel Synthetic and Natural Antidandruff Agents
Current Medicinal Chemistry Diagnostic Performance of Radiology Residents in Thoracic CT Imaging in Emergency Radiology During The COVID-19 Pandemic
Current Medical Imaging Prescription Patterns and Compliance with Antimicrobial Stewardship Team Recommendations Among Physicians in a Private Hospital in United Arab Emirates
New Emirates Medical Journal Plant Pathogenesis-Related Proteins PR-10 and PR-14 as Components of Innate Immunity System and Ubiquitous Allergens
Current Medicinal Chemistry Motor Unit and Neuromuscular Junction Remodeling with Aging
Current Aging Science A Survey of Recent Patents on CB2 Agonists in the Management of Pain
Recent Patents on CNS Drug Discovery (Discontinued) 5-HT7 Receptor Ligands: Recent Developments and Potential Therapeutic Applications
Mini-Reviews in Medicinal Chemistry COVID-19-associated Coagulopathy and Thromboembolism: Determination of Their Patterns and Risk Factors as Predictors of Mortality Among Severe COVID-19 Patients
Current Vascular Pharmacology Mechanism of Actions of Dexamethasone Against COVID-19 Predicted by Alpha Shape Analysis of Binding Sites
Current Bioinformatics Discovery of Anticancer Agents from 2-Pyrazoline-Based Compounds
Current Medicinal Chemistry Recent Medicinal Chemistry Approach for the Development of Dipeptidyl Peptidase IV Inhibitors
Current Medicinal Chemistry Synthesis and Antiviral Activity of Dihydropyrimidines - Ciprofloxacin Mannich bases Against Various Viral Strains
Anti-Infective Agents Bioisosteric Replacement and Related Analogs in the Design, Synthesis and Evaluation of Ligands for Muscarinic Acetylcholine Receptors
Medicinal Chemistry Star Graphs of Protein Sequences and Proteome Mass Spectra in Cancer Prediction
Current Proteomics How to Keep Oxidative Stress Under Control?
Current Nutrition & Food Science Recent Developments on Coronavirus Main Protease/3C Like Protease Inhibitors
Recent Patents on Anti-Infective Drug Discovery