Abstract
Antimitotics binding at the colchicine site of tubulin are important antitumour and vascular disrupting agents. Pyridines and azines are privileged scaffolds in medicinal chemistry and in recent years many colchicine site ligands (CSL) have incorporated them into their structures with the aim of improving their pharmacokinetic and pharmacodynamics properties. CSL have been classified according to their chemical structures and the chemical structures of the pyridine and azine containing antimitotic compounds are described. The designed principles behind the structural modifications and the achieved effect on the biological activity upon inclusion of these heterocycles are also discussed. Lessons from the achievements and failures have been extracted and future perspectives delineated.
Keywords: Pyridine, azines, antimitotics, tubulin, colchicine, antitumour, drug design.
Current Medicinal Chemistry
Title:Pyridine Based Antitumour Compounds Acting at the Colchicine Site
Volume: 23 Issue: 11
Author(s): R. Álvarez, L. Aramburu, P. Puebla, E. Caballero, M. González, A. Vicente, M. Medarde and R. Peláez
Affiliation:
Keywords: Pyridine, azines, antimitotics, tubulin, colchicine, antitumour, drug design.
Abstract: Antimitotics binding at the colchicine site of tubulin are important antitumour and vascular disrupting agents. Pyridines and azines are privileged scaffolds in medicinal chemistry and in recent years many colchicine site ligands (CSL) have incorporated them into their structures with the aim of improving their pharmacokinetic and pharmacodynamics properties. CSL have been classified according to their chemical structures and the chemical structures of the pyridine and azine containing antimitotic compounds are described. The designed principles behind the structural modifications and the achieved effect on the biological activity upon inclusion of these heterocycles are also discussed. Lessons from the achievements and failures have been extracted and future perspectives delineated.
Export Options
About this article
Cite this article as:
Álvarez R., Aramburu L., Puebla P., Caballero E., González M., Vicente A., Medarde M. and Peláez R., Pyridine Based Antitumour Compounds Acting at the Colchicine Site, Current Medicinal Chemistry 2016; 23 (11) . https://dx.doi.org/10.2174/092986732311160420104823
DOI https://dx.doi.org/10.2174/092986732311160420104823 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
- 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
-
Connexins as Precocious Markers and Molecular Targets for Chemical and Pharmacological Agents in Carcinogenesis
Current Medicinal Chemistry EDITORIAL [Hot topic: RAS - A Central Feature in Cancer Targeted Therapy (Guest Editor: Balazs Gyorffy)
Current Cancer Drug Targets Challenges and Opportunities in Molecular Imaging
Current Medical Imaging Vascular Endothelial Growth Factor and Its Receptor as Drug Targets in Hematological Malignancies
Current Drug Targets Antibody Fragments as Potential Biopharmaceuticals for Cancer Therapy: Success and Limitations
Current Medicinal Chemistry Application of Nanotechnology in the Diagnosis and Therapy of Hepatocellular Carcinoma
Recent Patents on Anti-Cancer Drug Discovery Stem Cells as In Vitro Models of Disease
Current Stem Cell Research & Therapy Recent Advances in Receptor-Targeted Fluorescent Probes for In Vivo Cancer Imaging
Current Medicinal Chemistry Anti-Cancer Cytotoxic Effects of Multiwalled Carbon Nanotubes
Current Pharmaceutical Design Targeting the Epidermal Growth Factor Receptor in Glioblastoma Treatment
Current Signal Transduction Therapy Current Phthalocyanines Delivery Systems in Photodynamic Therapy: An Updated Review
Current Medicinal Chemistry Production and Application of Copper Radiopharmaceuticals
Current Radiopharmaceuticals Germacrone: A Potent Secondary Metabolite with Therapeutic Potential in Metabolic Diseases, Cancer and Viral Infections
Current Drug Metabolism Beyond the "Lock and Key" Paradigm: Targeting Lipid Rafts to Induce the Selective Apoptosis of Cancer Cells
Current Medicinal Chemistry Phenolic Compounds as Nutraceuticals or Functional Food Ingredients
Current Pharmaceutical Design The Ubiquitin-Proteasome System (UPS) and the Mechanism of Action of Bortezomib
Current Pharmaceutical Design Antineoplastic Activity of Monocrotaline Against Hepatocellular Carcinoma
Anti-Cancer Agents in Medicinal Chemistry Cancer Diagnosis and Treatment Guidance: Role of MRI and MRI Probes in the Era of Molecular Imaging
Current Pharmaceutical Biotechnology Therapy Based on the Regulation of Thiol-dependent Redox Systems
Current Medicinal Chemistry Potential Deployment of Angiotensin I Converting Enzyme Inhibitors and of Angiotensin II Type 1 and Type 2 Receptor Blockers in Cancer Chemotherapy
Anti-Cancer Agents in Medicinal Chemistry