C10-aminoderivatives of colchicine: synthesis, structure and biological activity
Aĭtozhina, N.A.; Esbolaev, E.O.; Zubenko, T.A.; Toĭbaeva, K.A.; Aleksandrova, L.A.
Bioorganicheskaia Khimiia 22(5): 383-386
1996
ISSN/ISBN: 0132-3423 PMID: 8929225 Document Number: 458952
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.