Abstract
Imidazoles and benzimidazoles are privileged heterocyclic bioactive compounds used with success in the clinical practice of innumerous diseases. Although there are many advancements in cancer therapy, microtubules remain as one of the few macromolecular targets validated for planning active anti-cancer compounds, and the design of drugs that modulate microtubule dynamics in unknown sites of tubulin is one of the goals of the medicinal chemistry. The discussion of the role of new and commercially available imidazole and benzimidazole derivatives as tubulin modulators is scattered throughout scientific literature, and indicates that these compounds have a tubulin modulation mechanism different from that of tubulin modulators clinically available, such as paclitaxel, docetaxel, vincristine and vinblastine. In fact, recent literature indicates that these derivatives inhibit microtubule formation binding to the colchicine site, present good pharmacokinetic properties and are capable of overcoming multidrug resistance in many cell lines. The understanding of the mechanisms involved in the imidazoles/benzimidazoles modulation of microtubule dynamics is very important to develop new strategies to overcome the resistance to anti-cancer drugs and to discover new biomarkers and targets for cancer chemotherapy.
Keywords: Anti-tumour, benzimidazole, colchicine-binding site, imidazole, reposition of old drugs, tubulin.
Current Medicinal Chemistry
Title:Imidazoles and Benzimidazoles as Tubulin-Modulators for Anti-Cancer Therapy
Volume: 22 Issue: 11
Author(s): Fernando C. Torres, M. Eugenia Garcia-Rubino, Cesar Lozano-Lopez, Daniel F. Kawano, Vera L. Eifler-Lima, Gilsane L. von Poser and Joaquin M. Campos
Affiliation:
Keywords: Anti-tumour, benzimidazole, colchicine-binding site, imidazole, reposition of old drugs, tubulin.
Abstract: Imidazoles and benzimidazoles are privileged heterocyclic bioactive compounds used with success in the clinical practice of innumerous diseases. Although there are many advancements in cancer therapy, microtubules remain as one of the few macromolecular targets validated for planning active anti-cancer compounds, and the design of drugs that modulate microtubule dynamics in unknown sites of tubulin is one of the goals of the medicinal chemistry. The discussion of the role of new and commercially available imidazole and benzimidazole derivatives as tubulin modulators is scattered throughout scientific literature, and indicates that these compounds have a tubulin modulation mechanism different from that of tubulin modulators clinically available, such as paclitaxel, docetaxel, vincristine and vinblastine. In fact, recent literature indicates that these derivatives inhibit microtubule formation binding to the colchicine site, present good pharmacokinetic properties and are capable of overcoming multidrug resistance in many cell lines. The understanding of the mechanisms involved in the imidazoles/benzimidazoles modulation of microtubule dynamics is very important to develop new strategies to overcome the resistance to anti-cancer drugs and to discover new biomarkers and targets for cancer chemotherapy.
Export Options
About this article
Cite this article as:
Torres C. Fernando, Garcia-Rubino Eugenia M., Lozano-Lopez Cesar, Kawano F. Daniel, Eifler-Lima L. Vera, Poser L. von Gilsane and Campos M. Joaquin, Imidazoles and Benzimidazoles as Tubulin-Modulators for Anti-Cancer Therapy, Current Medicinal Chemistry 2015; 22 (11) . https://dx.doi.org/10.2174/0929867322666150114164032
DOI https://dx.doi.org/10.2174/0929867322666150114164032 |
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
-
High Throughput Determination of Gains and Losses of Genetic Material Using High Resolution BAC Arrays and Comparative Genomic Hybridization
Combinatorial Chemistry & High Throughput Screening Recent Trends in Nanotechnology-Based Drugs and Formulations for Targeted Therapeutic Delivery
Recent Patents on Inflammation & Allergy Drug Discovery Opioid Receptor Interacting Proteins and the Control of Opioid Signaling
Current Pharmaceutical Design Therapeutic Targets for Metastatic Prostate Cancer
Current Drug Targets Tumour Gene Therapy Monitoring Using Magnetic Resonance Imaging and Spectroscopy
Current Gene Therapy Cytotoxic, Antiproliferative and Apoptotic Effects of New Benzimidazole Derivatives on A549 Lung Carcinoma and C6 Glioma Cell Lines
Anti-Cancer Agents in Medicinal Chemistry The Role of 4-Thiazolidinone Scaffold in Targeting Variable Biomarkers and Pathways Involving Cancer
Anti-Cancer Agents in Medicinal Chemistry Leukocyte P2 Receptors: A Novel Target for Anti-inflammatory and Antitumor Therapy
Current Drug Targets - Cardiovascular & Hematological Disorders Targeting Cell Death in Tumors by Activating Caspases
Current Cancer Drug Targets Human Amnion–Derived Cells as a Reliable Source of Stem Cells
Current Molecular Medicine Targeted Angiogenesis Therapy in Head and Neck Squamous Cell Carcinomas
Current Angiogenesis (Discontinued) The Endothelin Axis as Therapeutic Target in Human Malignancies: Present and Future
Current Pharmaceutical Design SANTAVAC ™: A Novel Universal Antigen Composition for Developing Cancer Vaccines
Recent Patents on Biotechnology RNA Interference in Cancer: Targeting the Anti-Apoptotic Protein c-FLIP for Drug Discovery
Mini-Reviews in Medicinal Chemistry Application of Targeted Therapy to Malignant Gliomas and Response to Treatment
Current Signal Transduction Therapy Altered Hyaluronan Biosynthesis and Cancer Progression: an Immunological Perspective
Mini-Reviews in Medicinal Chemistry Viral Based Gene Therapy for Prostate Cancer
Current Gene Therapy Telomere Maintenance as Therapeutic Target in Embryonal Tumours
Anti-Cancer Agents in Medicinal Chemistry Nanoscale Formulations and Diagnostics With Their Recent Trends: A Major Focus of Future Nanotechnology
Current Pharmaceutical Design Small Molecules Targeting Mutant P53: A Promising Approach for Cancer Treatment
Current Medicinal Chemistry