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
-
Molecular Aspects of FKBP51 that Enable Melanoma Dissemination
Current Molecular Pharmacology Phytoconstituents of <i>Lantana camara</i> L.: Rekindling Hope in the Cancer Treatment
Current Bioactive Compounds Amino Acid Degrading Enzymes and their Application in Cancer Therapy
Current Medicinal Chemistry Ketogenic Diet Acts on Body Remodeling and MicroRNAs Expression Profile
MicroRNA Human- and Virus-Encoded microRNAs as Potential Targets of Antiviral Therapy
Mini-Reviews in Medicinal Chemistry The Emerging Role of EMT-related lncRNAs in Therapy Resistance and their Applications as Biomarkers
Current Medicinal Chemistry Lipoic Acid: A Novel Therapeutic Approach for Multiple Sclerosis and Other Chronic Inflammatory Diseases of the CNS
Endocrine, Metabolic & Immune Disorders - Drug Targets Reconceptualizing Adult Neurogenesis: Role for Sphingosine-1-Phosphate and Fibroblast Growth Factor-1 in Co-Ordinating Astrocyte-Neuronal Precursor Interactions
CNS & Neurological Disorders - Drug Targets Fluorescein Fluorescence Use in the Management of Intracranial Neoplastic and Vascular Lesions: A Review and Report of a New Technique
Current Drug Discovery Technologies Monoclonal Antibodies as Cancer Therapeutics
Recent Patents on Biotechnology Nanoemulsions for Improved Efficacy of Phytotherapeutics- A Patent Perspective
Recent Patents on Nanotechnology APE1/Ref-1Role in Redox Signaling: Translational Applications of Targeting the Redox Function of the DNA Repair/Redox Protein APE1/Ref-1
Current Molecular Pharmacology Clinical Update: Treatment of Glioblastoma Multiforme with Radiolabeled Antibodies that Target Tumor Necrosis
Current Cancer Therapy Reviews Hypoxia in Du-145 Prostate Cancer Xenografts After Estramustine Phosphate and Radiotherapy
Current Radiopharmaceuticals Histone Modifications as Molecular Targets in Nasopharyngeal Cancer
Current Medicinal Chemistry Intracellular Drug Delivery: Mechanisms for Cell Entry
Current Pharmaceutical Design A Prooxidant Mechanism for the Anticancer and Chemopreventive Properties of Plant Polyphenols
Current Drug Targets Evaluation of Biological Effects and Toxicity of Cetyltrimethylammonium Bromide Stabilized Silver Nanoparticles and Cetyltrimethylammonium Bromide Alone Following Intravenous Injection in Mice
Current Nanomedicine Green Tea Catechins as Novel Antitumor and Antiangiogenic Compounds
Current Medicinal Chemistry - Anti-Cancer Agents Catatonia, Malignant Catatonia, and Neuroleptic Malignant Syndrome
Current Psychiatry Reviews