Chemical Stability of the Peroxide Bond Enables Diversified Synthesis of Potent Tetraoxane Antimalarials
Identifieur interne : 001948 ( Main/Exploration ); précédent : 001947; suivant : 001949Chemical Stability of the Peroxide Bond Enables Diversified Synthesis of Potent Tetraoxane Antimalarials
Auteurs : Igor Opsenica [Serbie] ; Dejan Opsenica [Serbie] ; Kirsten S. Smith [Serbie] ; Wilbur K. Milhous [Serbie] ; Bogdan A. Šolaja [Serbie]Source :
- Journal of Medicinal Chemistry [ 0022-2623 ] ; 2008.
Abstract
Of 17 prepared 1,2,4,5-tetraoxacyclohexanes stable to reductive and acidic conditions, 3 of them were more active than artemisinin against CQ and MFQ resistant strain TM91C235 and all compounds were more active in vitro against W2 than against D6 strain. In vivo, amines 10 and 11a cured all mice at higher doses with MCD ≤ 37.5 (mg/kg)/day. Triol 13 was exceptionally active against melanoma (LOX IMVI) and ovarian cancer (IGROV1), both with LC50 = 60 nM.
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DOI: 10.1021/jm701417a
Affiliations:
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Chem.</title><idno type="ISSN">0022-2623</idno><idno type="eISSN">1520-4804</idno><imprint><publisher>American Chemical Society</publisher><date type="e-published" when="2008-03-11">2008</date><date when="2008-04-10">2008</date><biblScope unit="vol">51</biblScope><biblScope unit="issue">7</biblScope><biblScope unit="page" from="2261">2261</biblScope><biblScope unit="page" to="2266">2266</biblScope></imprint><idno type="ISSN">0022-2623</idno></series></biblStruct></sourceDesc><seriesStmt><idno type="ISSN">0022-2623</idno></seriesStmt></fileDesc><profileDesc><textClass></textClass></profileDesc></teiHeader><front><div type="abstract">Of 17 prepared 1,2,4,5-tetraoxacyclohexanes stable to reductive and acidic conditions, 3 of them were more active than artemisinin against CQ and MFQ resistant strain TM91C235 and all compounds were more active in vitro against W2 than against D6 strain. In vivo, amines 10 and 11a cured all mice at higher doses with MCD ≤ 37.5 (mg/kg)/day. 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