مورد إلكتروني
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.
| العنوان: | 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. |
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| المؤلفون: | 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 |
| المصدر: | Journal of medicinal chemistry, 48 (3 |
| بيانات النشر: | 2005-02 |
| نوع الوثيقة: | Electronic Resource |
| مستخلص: | 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. Journal Article Research Support, Non-U.S. Gov't info:eu-repo/semantics/published |
| مصطلحات الفهرس: | Sciences bio-médicales et agricoles, Animals, Antineoplastic Agents -- chemical synthesis, Antineoplastic Agents -- isolation & purification, Antineoplastic Agents -- pharmacology, Calotropis -- chemistry, Camptothecin -- analogs & derivatives, Camptothecin -- pharmacology, Cardenolides -- chemical synthesis, Cardenolides -- isolation & purification, Cardenolides -- pharmacology, Cell Line, Tumor, Cell Proliferation -- drug effects, Cerebral Cortex -- chemistry, Drug Resistance, Multiple, Drug Resistance, Neoplasm, Drug Screening Assays, Antitumor, Etoposide -- pharmacology, Humans, Magnetic Resonance Spectroscopy, Maximum Tolerated Dose, Mice, Organoplatinum Compounds -- pharmacology, Paclitaxel -- pharmacology, Sodium-Potassium-Exchanging ATPase -- chemistry, Structure-Activity Relationship, Swine, Thiazoles -- chemical synthesis, Thiazoles -- isolation & purification, Thiazoles -- pharmacology, info:eu-repo/semantics/article, info:ulb-repo/semantics/articlePeerReview, info:ulb-repo/semantics/openurl/article |
| URL: | |
| الإتاحة: | Open access content. Open access content |
| ملاحظة: | No full-text files English |
| أرقام أخرى: | EQY oai:dipot.ulb.ac.be:2013/52110 uri/info:doi/10.1021/jm049405a uri/info:pmid/15689169 uri/info:scp/20044369153 778634799 |
| المصدر المساهم: | UNIVERSITE LIBRE DE BRUXELLES From OAIster®, provided by the OCLC Cooperative. |
| رقم الأكسشن: | edsoai.ocn778634799 |
| قاعدة البيانات: | OAIster |
| الوصف غير متاح. |