Synthesis and cytotoxic evaluation of new colchicine derivatives bearing 1,3,4-thiadiazole moieties

In search of novel anticancer agents, a series of N-methyl colchiceinamide derivatives (7a–7i) containing 1,3,4-thiadiazole moieties were synthesized, and their structures were confirmed by spectral analysis. Cytotoxicity of these compounds was evaluated by MTT assay in vitro against four human tumor cell lines, i.e. A2780, A549, BEL7402, and MCF-7. The results indicated that most of the derivatives showed significant anticancer activities, particularly, compounds 7h and 7i showed more potent cytotoxic activities of all screened cancer cells than colchicine.

Graphical abstractA series of novel colchicine derivatives bearing 1,3,4-thiadiazole moieties were synthesized and evaluated for their cytotoxicity against four human tumor cell lines. Compounds 7h and 7i showed more potent cytotoxic activities of all screened cancer cells.Figure optionsDownload full-size imageDownload as PowerPoint slide