Biochemical Pharmacology volume 77, issue 3, P322-336 2009 DOI: 10.1016/j.bcp.2008.10.015 View full text
Carmony L. Hartwig, Andrew S. Rosenthal, John D’Angelo, Carol E. Griffin, Gary H. Posner, Roland A. Cooper

Abstract: AbstractThe antimalarial trioxanes, exemplified by the naturally occurring sesquiterpene lactone artemisinin and its semi-synthetic derivatives, contain an endoperoxide pharmacophore that lends tremendous potency against Plasmodium parasites. Despite decades of research, their mechanism of action remains unresolved. A leading model of anti-plasmodial activity hypothesizes that iron-mediated cleavage of the endoperoxide bridge generates cytotoxic drug metabolites capable of damaging cellular macromolecules. To…

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