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Mixed tetraoxanes containing the acetone subunit as antimalarials

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2008
Authors
Opsenica, Dejan
Terzić-Jovanović, Nataša
Smith, P.L.
Yang, Y.
Anova, L.
Smith, K. S.
Šolaja, Bogdan
Article (Published version)
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Abstract
Eleven new tetraoxanes possessing cholic acid-derived carrier and isopropylidene moiety were synthesized and were tested in vitro and in vivo. In vitro screening revealed that nine of them were more potent against CQ-resistant W2 than CQ-susceptible D6 strain and that two of them were equally or more potent than artemisinin and mefloquine against multi-drug resistant TM91C235 strain. Amine 8 cured all mice at the dose of 160 mg/kg/day, while the anilide 9 exhibited MCD ≤ 20 mg/kg/day. The diol 13 was most potent antiproliferative with GI50, TGI, LC50 MG_MID 0.98 μM, 3.80 μM, 11.22 μM, respectively. All tested compounds showed no toxic effects.
Keywords:
Antimalarials / Antiproliferatives / Cholic acid / Metabolic stability / Mixed steroidal tetraoxanes
Source:
Bioorganic and Medicinal Chemistry, 2008, 16, 14, 7039-7045
Publisher:
  • Pergamon-Elsevier Science Ltd, Oxford
Projects:
  • Peroksidni antimalarici i njihove himere sa hinolinima: sinteza i biološka aktivnost (RS-142022)

DOI: 10.1016/j.bmc.2008.05.017

ISSN: 0968-0896

PubMed: 18550377

WoS: 000257829600042

Scopus: 2-s2.0-48949115566
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URI
http://cer.ihtm.bg.ac.rs/handle/123456789/444
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