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J Med Chem. 2007 Oct 18;50(21):5118-27. Epub 2007 Sep 21.

Deoxycholic acid-derived tetraoxane antimalarials and antiproliferatives(1).

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  • 1Institute of Chemistry, Technology and Metallurgy, Belgrade, Serbia.


The synthesis of deoxycholic acid (DCA)- and cholic acid (CA)-derived mixed tetraoxanes revealed that N-(2-dimethylamino)ethyl derivatives are potent antimalarials in vitro and in vivo. The tetraoxanes presented in this paper are dual inhibitors: besides curing mice in vivo without observed toxic effects, they kill cancer cell lines at very low concentrations. For example, DCA and CA derivatives 16 and 25 cured 3/5 (160 mg/kg/day) and 2/5 (40 mg/kg/day, MTD >960 mg/kg), respectively, and they were extremely active against melanoma LOX IMVI cancer, LC50 = 22 nM and 69 nM, respectively.

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