Deoxycholic acid-derived tetraoxane antimalarials and antiproliferatives
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Smith, K. S.
Milhous, Wilbur K.
Article (Published version)
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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.
Source:Journal of Medicinal Chemistry, 2007, 50, 21, 5118-5127
- Amer Chemical Soc, Washington