Homologous series of novel adamantane–colchicine conjugates: synthesis and cytotoxic effect on human cancer cellsстатья
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Дата последнего поиска статьи во внешних источниках: 4 сентября 2018 г.
Аннотация:A series of homologues of N-(7-(adamant-1-yloxy)-7-heptanoyl)-N-deacetylcolchicine (1a) with sequential shift of the ester group in the chain connecting colchicine and adamantane moieties was synthesized to find an optimal position of this group. All homologues possessed very high cytotoxicity to human lung carcinoma cell line A549 demonstrating a weak dependence of toxic activity on the ester group position. The cytotoxicity of the most active compound (7a, EC50=5.9 nM) was close to that of clinically used anti-tubulin anticancer drug taxol.