Anticancer and Antimalarial Efficacy and Safety of Artemisinin-Derived Trioxane Dimers in Rodents
| Autor: | and Adebusola Alagbala, Andrew J. McRiner, Suji Xie, Ik-Hyeon Paik, Barbara A. Foster, Gary H. Posner, Surojit Sur, Theresa A. Shapiro, Kristina Borstnik |
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| Rok vydání: | 2004 |
| Předmět: |
Male
Trioxane Stereochemistry Dimer Plasmodium falciparum Drug Resistance Administration Oral Antineoplastic Agents Adenocarcinoma Chemical synthesis Antimalarials Mice Structure-Activity Relationship chemistry.chemical_compound Oral administration Cell Line Tumor Drug Discovery medicine Animals Structure–activity relationship Artemisinin biology Prostatic Neoplasms Flow Cytometry biology.organism_classification Artemisinins chemistry Artesunate Injections Intravenous Molecular Medicine Drug Screening Assays Antitumor Dimerization medicine.drug |
| Zdroj: | Journal of Medicinal Chemistry. 47:1299-1301 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm0303711 |
| Popis: | In only four chemical steps from naturally occurring artemisinin (1), trioxane dimers 6 and 7 were prepared on a multigram scale in overall 32-44% yields. In mice, both isonicotinate N-oxide dimer 6 and isobutyric acid dimer 7 were considerably more antimalarially efficacious than clinically used sodium artesunate (2) via both oral and intravenous administration. In the transgenic adenocarcinoma of mouse prostate model, some of the trioxane dimers had potent anticancer activity. |
| Databáze: | OpenAIRE |
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