Deoxycholic acid-derived tetraoxane antimalarials and antiproliferatives(1).
Copyright policy )Deoxycholic acid-derived tetraoxane antimalarials and antiproliferatives(1).
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.
- Moldova State University Moldova (Republic of)
- Moldova State University, Institute of Chemistry Moldova (Republic of)
Plasmodium berghei, Plasmodium falciparum, Drug Resistance, Antineoplastic Agents, Stereoisomerism, Crystallography, X-Ray, Malaria, Antimalarials, Mice, Structure-Activity Relationship, Cyclohexanes, Cell Line, Tumor, Microsomes, Animals, Humans, Drug Screening Assays, Antitumor, Tetraoxanes, Deoxycholic Acid
Plasmodium berghei, Plasmodium falciparum, Drug Resistance, Antineoplastic Agents, Stereoisomerism, Crystallography, X-Ray, Malaria, Antimalarials, Mice, Structure-Activity Relationship, Cyclohexanes, Cell Line, Tumor, Microsomes, Animals, Humans, Drug Screening Assays, Antitumor, Tetraoxanes, Deoxycholic Acid
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