Chemical Stability of the Peroxide Bond Enables Diversified Synthesis of Potent Tetraoxane Antimalarials (1)

I Opsenica, D Opsenica, KS Smith…

文献索引：Opsenica, Igor; Opsenica, Dejan; Smith, Kirsten S.; Milhous, Wilbur K.; Solaja, Bogdan A. Journal of Medicinal Chemistry, 2008 , vol. 51, # 7 p. 2261 - 2266

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被引用次数: 58

摘要

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 ...