Identification of a Novel Cardenolide (2‘ ‘-Oxovoruscharin) from Calotropis p rocera and the Hemisynthesis of Novel Derivatives Displaying Potent in Vitro Antitumor Activities and High in Vivo Tolerance: Structure−Activity Relationship Analyses
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...
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| Veröffentlicht in: | Journal of medicinal chemistry 2005-02, Vol.48 (3), p.849-856 |
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| container_title | Journal of medicinal chemistry |
| container_volume | 48 |
| creator | Van Quaquebeke, Eric Simon, Gentiane André, Aurélie Dewelle, Janique Yazidi, Mohamed El Bruyneel, Frederic Tuti, Jerome Nacoulma, Odile Guissou, Pierre Decaestecker, Christine Braekman, Jean-Claude Kiss, Robert Darro, Francis |
| description | 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. |
| doi_str_mv | 10.1021/jm049405a |
| format | Article |
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Med. Chem</addtitle><description>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. 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Med. Chem</addtitle><date>2005-02-10</date><risdate>2005</risdate><volume>48</volume><issue>3</issue><spage>849</spage><epage>856</epage><pages>849-856</pages><issn>0022-2623</issn><eissn>1520-4804</eissn><abstract>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.</abstract><pub>American Chemical Society</pub><doi>10.1021/jm049405a</doi><tpages>8</tpages></addata></record> |
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| source | American Chemical Society Journals |
| title | Identification of a Novel Cardenolide (2‘ ‘-Oxovoruscharin) from Calotropis p rocera and the Hemisynthesis of Novel Derivatives Displaying Potent in Vitro Antitumor Activities and High in Vivo Tolerance: Structure−Activity Relationship Analyses |
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