Abstract
New analogues of anticancer agent tubuloclustin N-[7-(adamantan-1-yloxy)-7-heptanoyl]-N-deacetylcolchicine with ether moiety in the linker between colchicine and adamantine fragments were synthesized from w-(adamantan-1-yloxy)alkan- 1-ols. These compounds effectively inhibited growth of human lung carcinoma cell line A549 (IC50 = 5–15.5 nM), induced both apoptosis and formation of tubulin clusters. The conjugates lacking ester carbonyl in the linker exhibit improved metabolic stability and are promising for further cytotoxicity studies in vivo.
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