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  • Title: Design, synthesis, and biological evaluation of biotinylated colchicine derivatives as potential antitumor agents.
    Author: Wang C, Zhang Y, Wang Z, Li Y, Guan Q, Xing D, Zhang W.
    Journal: J Enzyme Inhib Med Chem; 2022 Dec; 37(1):411-420. PubMed ID: 34915785.
    Abstract:
    Chemical drug design based on the biochemical characteristics of cancer cells has become an important strategy for discovering new anti-tumour drugs to improve tumour targeting effects and reduce off-target toxicities. Colchicine is one of the most prominent and historically microtubule-targeting drugs, but its clinical applications are hindered by notorious adverse effects. In this study, we presented a novel tumour-specific conjugate 9 that consists of deacetylcolchicine (Deac), biotin, and a cleavable disulphide linker. 9 was found to exhibit potent anti-tumour activity and exerted higher selectivity between tumour and nontarget cells than Deac. The targeting moiety biotin might enhance the transport capability and selectivity of 9 to tumour cells via biotin receptor-mediated endocytosis. The tubulin polymerisation activity of 9 (with DTT) was close to the parent drug Deac. These preliminary results suggested that 9 is a high potency and reduced toxicity antitumor agent and worthy of further investigation.
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