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Deoxycholic acid-derived tetraoxane antimalarials and antiproliferatives

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2007
Authors
Terzić-Jovanović, Nataša
Opsenica, Dejan
Milić, Dragana
Tinant, Bernard
Smith, K. S.
Milhous, Wilbur K.
Šolaja, Bogdan
Article (Published version)
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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.
Source:
Journal of Medicinal Chemistry, 2007, 50, 21, 5118-5127
Publisher:
  • Amer Chemical Soc, Washington
Projects:
  • Peroksidni antimalarici i njihove himere sa hinolinima: sinteza i biološka aktivnost (RS-142022)

DOI: 10.1021/jm070684m

ISSN: 0022-2623

PubMed: 17887664

WoS: 000250110700009

Scopus: 2-s2.0-35348910826
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URI
http://cer.ihtm.bg.ac.rs/handle/123456789/350
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