- Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids.
Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids.
European journal of medicinal chemistry (2017-10-14)
Ekaterina S Shchegravina, Alexander A Maleev, Stanislav K Ignatov, Iuliia A Gracheva, Andreas Stein, Hans-Günther Schmalz, Andrey E Gavryushin, Anastasiya A Zubareva, Elena V Svirshchevskaya, Alexey Yu Fedorov
PMID29028531
摘要
Two novel indole-containing allocolchicinoids were prepared from naturally occurring colchicine exploiting the Curtius rearrangement and tandem Sonogashira coupling/Pd-catalyzed cyclization as the key transformations. Their cytotoxic properties, apoptosis-inducing activity, tubulin assembly inhibition and short-time cytotoxic effects were investigated. Compound 7 demonstrated the most pronounced anti-cancer activity: IC
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