[C10-aminoderivatives of colchicine: synthesis, structure and biological activity]

Replacement of the 10-methoxy group of colchicine by amino and amino acid substituents sharply decreased its toxicity and only slightly decreased its tubulin-binding activity, and thus, gave rise to a number of weakly toxic colchicine analogs. In particular, highly active 10-(N-glycino)-10-demethoxycolchicine and 10-[N-(beta-alanino)]-10-demethoxycolchicine were prepared.