Colchicine Alkaloids and Synthetic Analogues: Current Progress and Perspectives

J Med Chem. 2020 Oct 8;63(19):10618-10651. doi: 10.1021/acs.jmedchem.0c00222.

Iuliia A Gracheva ¹, Ekaterina S Shchegravina ¹, Hans-Günther Schmalz ², Irina P Beletskaya ³, Alexey Yu Fedorov ¹

Affiliations

1 Department of Chemistry, Lobachevsky State University of Nizhny Novgorod, Nizhny Novgorod 603950, Russian Federation.
2 Department of Chemistry, University of Cologne, 50939 Cologne, Germany.
3 Department of Chemistry, M. V. Lomonosov Moscow State University, Moscow 119992, Russian Federation.

PMID: 32432867 DOI: 10.1021/acs.jmedchem.0c00222

Abstract

Colchicine, the main alkaloid of Colchicum autumnale, is one of the most famous natural molecules. Although colchicine belongs to the oldest drugs (in use since 1500 BC), its pharmacological potential as a lead structure is not yet fully exploited. This review is devoted to the synthesis and structure-activity relationships (SAR) of colchicine Alkaloids and their analogues with modified A, B, and C rings, as well as hybrid compounds derived from colchicinoids including prodrugs, conjugates, and delivery systems. The systematization of a vast amount of information presented to date will create a paradigm for future studies of colchicinoids for neoplastic and various Other Diseases.

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