Abstract
In this paper we provide an overview of the status of various colchicine derivatives in preclinical development with special focus on their anti-cancer activity. We discuss several groups of compounds that have been designed to differentially bind with specific affinities for tubulin β isotypes, especially in regard to βIII, which is commonly over-expressed in cancer. Computational prediction, protein-based and cell-based assays are summarized as well as some animal tests conducted on these compounds. It is concluded that an untapped potential exists for exploiting the colchicine scaffold as a pharmacophore with the possibility of increasing its affinity for tubulin isotypes overexpressed in cancer and decreasing it for normal cells thereby widening the therapeutic window.
Keywords: Anti-cancer, Tubulin β isotypes, Colchicine Scaffold, Pharmacophore, Animal tests
Graphical Abstract
Current Topics in Medicinal Chemistry
Title:Novel Colchicine Derivatives and their Anti-cancer Activity
Volume: 17 Issue: 22
Author(s): Lorelei Johnson*, Ing Swie Goping, Aja Rieger, Jonathan Y. Mane, Torin Huzil, Asok Banerjee, Richard Luduena, Bashar Hassani, Philip Winter and Jack A. Tuszynski
Affiliation:
- Department of Oncology, University of Alberta, Edmonton, Alberta,Canada
Keywords: Anti-cancer, Tubulin β isotypes, Colchicine Scaffold, Pharmacophore, Animal tests
Abstract: In this paper we provide an overview of the status of various colchicine derivatives in preclinical development with special focus on their anti-cancer activity. We discuss several groups of compounds that have been designed to differentially bind with specific affinities for tubulin β isotypes, especially in regard to βIII, which is commonly over-expressed in cancer. Computational prediction, protein-based and cell-based assays are summarized as well as some animal tests conducted on these compounds. It is concluded that an untapped potential exists for exploiting the colchicine scaffold as a pharmacophore with the possibility of increasing its affinity for tubulin isotypes overexpressed in cancer and decreasing it for normal cells thereby widening the therapeutic window.
Export Options
About this article
Cite this article as:
Johnson Lorelei*, Goping Swie Ing, Rieger Aja, Mane Y. Jonathan, Huzil Torin, Banerjee Asok, Luduena Richard, Hassani Bashar, Winter Philip and Tuszynski A. Jack, Novel Colchicine Derivatives and their Anti-cancer Activity, Current Topics in Medicinal Chemistry 2017; 17 (22) . https://dx.doi.org/10.2174/1568026617666170104143618
DOI https://dx.doi.org/10.2174/1568026617666170104143618 |
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
-
Renal and Urological Diseases of the Newborn Neonatal Acute Kidney Injury
Current Pediatric Reviews Heart Failure in North America
Current Cardiology Reviews Modelling Chemotherapy-induced Cardiotoxicity by Human Pluripotent Stem Cells
Current Drug Targets Update on the Rheumatologic Manifestations of Malignancy
Current Cancer Therapy Reviews Evaluation of Echocardiographic Abnormalities in HIV Positive Patients Treated with Antiretroviral Medications
Infectious Disorders - Drug Targets Mycobacterium w Immunotherapy for Treating Pulmonary Tuberculosis - a Systematic Review
Current Pharmaceutical Design Immunopathological Aspects of Mycoplasma pneumoniae Infection
Current Pediatric Reviews Atrial Tachycardias Occurring Late After Open Heart Surgery
Current Cardiology Reviews Chemotherapy and Cardiotoxicity in Hematologic Malignancies
Current Cancer Drug Targets In Vivo Osteoarthritis Target Validation Utilizing Genetically-Modified Mice
Current Drug Targets Therapeutic Approach to Multiple Sclerosis by Novel Oral Drugs
Recent Patents on Inflammation & Allergy Drug Discovery Antineutrophil Cytoplasmic Antibody in Lupus Nephritis: Correlation with Clinicopathological Characteristics and Disease Activity
Current Rheumatology Reviews Pharmacological Characteristics and Clinical Applications of K201
Current Clinical Pharmacology Pharmacological Properties of Physical Exercise in The Elderly
Current Pharmaceutical Design Moving Troponin Testing into the 21st Century: Will Greater Sensitivity Be Met with Greater Sensibility?
Cardiovascular & Hematological Disorders-Drug Targets Tombstoning ST-Elevation Myocardial Infarction
Current Cardiology Reviews Pulmonary Involvement in Inflammatory Bowel Disease
Current Drug Targets - Inflammation & Allergy Tuberculosis Treated by Multiple Drugs: An Overview
Current Drug Delivery Cardiotoxicity of Molecularly Targeted Agents
Current Cardiology Reviews Deep Inspiration Breath-hold (DIBH) Technique to Reduce Cardiac Radiation Dose in the Management of Breast Cancer
Current Cancer Therapy Reviews