Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives
Iuliia A Gracheva1, Ekaterina S Shchegravina1, Hans-Günther Schmalz2
1Department of Chemistry, Lobachevsky State University of Nizhny Novgorod, Nizhny Novgorod 603950, Russian Federation.
Journal of Medicinal Chemistry
|May 21, 2020
Summary
Colchicine, an ancient natural alkaloid, offers significant untapped potential as a lead compound. This review explores its synthesis, structure-activity relationships, and novel derivatives for treating neoplastic and other diseases.
Area of Science:
- Natural Product Chemistry
- Medicinal Chemistry
- Pharmacology
Background:
- Colchicine, derived from *Colchicum autumnale*, is a historically significant natural product.
- Despite its long history of use, colchicine's full pharmacological potential remains underexplored.
- Its unique structure serves as a valuable scaffold for drug development.
Purpose of the Study:
- To review the synthesis and structure-activity relationships (SAR) of colchicine alkaloids and their analogs.
- To explore modified colchicinoids, including hybrid compounds, prodrugs, conjugates, and delivery systems.
- To establish a framework for future research into colchicinoids for various diseases, particularly cancer.
Main Methods:
- Literature review and systematization of existing data on colchicine and its derivatives.
- Analysis of structure-activity relationships based on modifications to the A, B, and C rings.
- Investigation of novel synthetic strategies and hybrid compound development.
Main Results:
- Detailed overview of synthetic routes for colchicine alkaloids and analogs.
- Comprehensive analysis of SAR, highlighting key structural features influencing activity.
- Identification of promising prodrugs, conjugates, and delivery systems for enhanced therapeutic applications.
Conclusions:
- Colchicine and its derivatives represent a rich source of potential therapeutic agents.
- Systematic understanding of SAR is crucial for optimizing drug design.
- Further research into colchicinoids holds promise for treating neoplastic and other diseases.
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