(-)-Colchicine, an anti-microtubulin polymerization agent, is a valuable medication and the drug of choice for gout, Behçet's disease and familial Mediterranean fever. It has a narrow therapeutic index due to its high toxicity towards normal cells. Nonetheless, numerous (-)-colchicine derivatives have been synthesized and studied for their structure-activity relationship and preferential toxicity. Different functional groups such as amides, thioamides, N-arylurea and 8,12-diene cyclic have been incorporated into (-)-colchicine, resulting in derivatives (with moieties) that include electron-withdrawing and electron-donating groups. This review article focuses on recent developments in the chemical synthesis of (-)-colchicine derivatives, the substituents used, the functional groups linked to the substituents, the moieties and biological studies. Moreover, the current classification of derivatives based on the (-)-colchicine rings, namely ring A, B, and C (-)-colchicine derivatives, is discussed. This work demonstrates and summarizes the significance of (-)-colchicine derivatives in the biological field, and discusses their promising therapeutics for the future.
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http://dx.doi.org/10.1016/j.ejmech.2019.111788 | DOI Listing |
Curr Top Med Chem
January 2025
GITAM School of Pharmacy, GITAM Deemed to be University, Rudraram, Patancheru, Sanga Reddy, Telangana-502329, India.
Background: Piperidines are among the essential synthetic fragments for designing drugs and play a significant role in the pharmaceutical industry. The synthesis of newer derivatives by incorporating different amines paves the way for the introduction of novel drug combinations for current cancer treatments.
Method: The new combinations of 1-(4-bromo-2-(pyrrolidine-1-yl) benzyl) piperidine derivatives were synthesized by adding various amino groups.
Plants (Basel)
November 2024
Zhejiang Provincial Key Laboratory of Plant Evolutionary Ecology and Conservation, School of Life Sciences, Taizhou University, Taizhou 318000, China.
Nakai ex F. Maek. has been employed in traditional Chinese medicine for millennia.
View Article and Find Full Text PDFActa Pharmacol Sin
December 2024
Anhui Provincial International Science and Technology Cooperation Base for Major Metabolic Diseases and Nutritional Interventions, Key Laboratory of Metabolism and Regulation for Major Diseases of Anhui Higher Education Institutes, School of Food and Biological Engineering, Hefei University of Technology, Hefei, 230601, China.
Vascular smooth muscle cell (VSMC) phenotype transformation significantly contributes to vascular intimal hyperplasia. However, effective preventive and therapeutic measures are lacking. Colchicine, a binary alkaloid derived from Colchicum autumnale, is traditionally used for treating inflammatory diseases.
View Article and Find Full Text PDFTheor Appl Genet
December 2024
Department of Agronomy, Iowa State University, Ames, IA, 50011, USA.
Restoration of haploid female and haploid male fertility without colchicine is feasible. Three SNPs and eight gene models for HFF, and one SNP and a gene model for HMF were identified. Doubled haploid (DH) breeding accelerates the development of elite inbred lines and facilitates the incorporation of exotic germplasm, offering a powerful tool for maize improvement.
View Article and Find Full Text PDFJ Stroke Cerebrovasc Dis
December 2024
Department of Clinical Neurological Sciences, Western University, London, Ontario, Canada. Electronic address:
Background: Stroke incidence remains a significant concern despite optimized prevention strategies. Colchicine shows potential for improving stroke prevention globally.
Aims: To summarize efficacy and safety estimates from systematic reviews and meta-analyses (SRMAs) of randomized controlled trials (RCTs) comparing colchicine to usual care or placebo for stroke prevention.
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