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  • Title: Deoxycholic acid-derived tetraoxane antimalarials and antiproliferatives(1).
    Author: Terzić N, Opsenica D, Milić D, Tinant B, Smith KS, Milhous WK, Solaja BA.
    Journal: J Med Chem; 2007 Oct 18; 50(21):5118-27. PubMed ID: 17887664.
    Abstract:
    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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