Department of Chemistry, Lobachevsky State University of Nizhny Novgorod, Nizhny Novgorod 603950, Russian Federation.
Department of Chemistry, University of Cologne, 50939 Cologne, Germany.
J Med Chem. 2020 Oct 8;63(19):10618-10651. doi: 10.1021/acs.jmedchem.0c00222. Epub 2020 Jun 4.
Colchicine, the main alkaloid of , 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.
秋水仙碱是百合科秋水仙属植物的主要生物碱之一,是最著名的天然分子之一。尽管秋水仙碱属于最古老的药物之一(自公元前 1500 年就开始使用),但其作为先导结构的药理学潜力尚未得到充分开发。本综述致力于合成和结构-活性关系(SAR)的秋水仙碱生物碱及其类似物与修改的 A、B 和 C 环,以及包括前药、缀合物和输送系统的来源于秋水仙碱的杂化合物。对迄今提出的大量信息进行系统整理,将为今后研究秋水仙碱类药物治疗肿瘤和各种其他疾病提供范例。