Anticancer and Antimalarial Efficacy and Safety of Artemisinin-Derived Trioxane Dimers in Rodents
Authors:
- Gary H. PosnerGPGary H. Posner
- Andrew J. McRinerAMAndrew J. McRiner
- Ik-Hyeon PaikIPIk-Hyeon Paik
- Surojit SurSSSurojit Sur
- Kristina BorstnikKBKristina Borstnik
- Suji XieSXSuji Xie
- Theresa A. ShapiroTSTheresa A. Shapiro
- Adebusola AlagbalaAAAdebusola Alagbala
- Barbara FosterBFBarbara Foster
- 31 January 2004
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 47 (5) , 1299-1301
Abstract
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.Keywords
This publication has 6 references indexed in Scilit:
- A Short Synthesis and Biological Evaluation of Potent and Nontoxic Antimalarial Bridged Bicyclic β-Sulfonyl-EndoperoxidesJournal of Medicinal Chemistry, 2003
- Orally Active, Antimalarial, Anticancer, Artemisinin-Derived Trioxane Dimers with High Stability and EfficacyJournal of Medicinal Chemistry, 2003
- Antitumor Activity of Novel Deoxoartemisinin Monomers, Dimers, and TrimerJournal of Medicinal Chemistry, 2003
- Malaria: New Chemotherapeutic Peroxide DrugsMini-Reviews in Medicinal Chemistry, 2002
- From Mechanistic Studies on Artemisinin Derivatives to New Modular Antimalarial DrugsAccounts of Chemical Research, 2002
- Inhibitory effects of the nucleoside analogue gemcitabine on prostatic carcinoma cellsThe Prostate, 1996