1. Deoxycholic Acid-Derived Tetraoxane Antimalarials and Antiproliferatives1.
- Author
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Nataša Terzi, Dejan Opsenica, Dragana Mili, Bernard Tinant, Kirsten S. Smith, Wilbur K. Milhous, and Bogdan A. Šolaja
- Subjects
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PAPER , *CHOLIC acid , *ANTIMALARIALS , *DIMETHYLAMINOETHANOL , *CANCER - 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 16and 25cured 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, LC5022 nM and 69 nM, respectively. [ABSTRACT FROM AUTHOR]
- Published
- 2007
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