Synthesis and in vitro antimalarial activity of tetraoxane-amine/amide conjugates

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• 作者：Nitin Kumar ; Shabana I. Khan ; Himanshu Atheaya ; Ritu Mamgain ; Diwan S. Rawat
• 关键词：Plasmodium falciparum ; Artemisinin ; Tetraoxane ; Amine conjugates
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：July 2011
• 年：2011
• 卷：46
• 期：7
• 页码：2816-2827
• 全文大小：341 K

文摘

A series of tetraoxanes, tetraoxane-amine and tetraoxane-amide conjugates have been synthesized and screened for in vitro antimalarial activity against chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. Most of the conjugates showed slightly better antimalarial activity than the parent tetraoxanes. Three of the conjugate compounds were potentially active with IC₅₀ values in the range of 0.38–0.80 μM. Cytotoxicity of four selected compounds was also evaluated in a panel of four cancer (SK-MEL, KB, BT-549, SK-OV-3) and two non-cancer (Vero and LLC-PK₁₁) cell lines up to a concentration of 25 μM and none of the compounds was found toxic to any of the cells.