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  • Title: Synthesis and biological evaluation of novel non-racemic indole-containing allocolchicinoids.
    Author: Shchegravina ES, Maleev AA, Ignatov SK, Gracheva IA, Stein A, Schmalz HG, Gavryushin AE, Zubareva AA, Svirshchevskaya EV, Fedorov AY.
    Journal: Eur J Med Chem; 2017 Dec 01; 141():51-60. PubMed ID: 29028531.
    Abstract:
    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: IC50 < 1 nM, cell cycle arrest in the G2/M phase, 25% apoptosis induction, as well as lower destructive short-time effects on HT-29 cell line in comparison with colchicine. Docking studies for prepared indole-derived allocolchicine analogues were carried out.
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