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Identification of a novel cardenolide (2''-oxovoruscharin) from Calotropis procera and the hemisynthesis of novel derivatives displaying potent in vitro antitumor activities and high in vivo tolerance: structure-activity relationship analyses.

par Van Quaquebeke, Eric ;Simon, Gentiane;André, Aurélie;Dewelle, Janique;El Yazidi, Mohamed ;Bruyneel, Frederic;Tuti, Jérôme;Nacoulma, Odile;Guissou, Pierre;Decaestecker, Christine ;Braekman, Jean Claude ;Kiss, Robert ;Darro, Francis
Référence Journal of medicinal chemistry, 48, 3, page (849-856)
Publication Publié, 2005-02

Article révisé par les pairs

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Résumé :

Analysis of the methanolic extract of Calotropis procera root barks enabled the identification of a novel cardenolide (2''-oxovoruscharin) to be made. Of the 27 compounds that we hemisynthesized, one (23) exhibited a very interesting profile with respect to its hemisynthetic chemical yield, its in vitro antitumor activity, its in vitro inhibitory influence on the Na+/K+-ATPase activity, and its in vivo tolerance. Compound 23 displayed in vitro antitumor activity on a panel of 57 human cancer cell lines similar to taxol, and higher than SN-38 (the active metabolite of irinotecan), two of the most potent drugs used in hospitals to combat cancer.