Atovaquone derivatives as potent cytotoxic and apoptosis inducing agents

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• 作者：Jing Zhou ; Lei Duan ; Huaming Chen ; Xiaomei Ren ; Zhang Zhang ; Fengtao Zhou ; Jinsong Liu ; Duanqing Pei ; Ke Ding
• 关键词：Atovaquone ; Apoptosis ; Cytotoxic
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：1 September 2009
• 年：2009
• 卷：19
• 期：17
• 页码：5091-5094
• 全文大小：322 K

文摘

2-Piperazinyl naphthoquinones (2) and 2-piperidinyl naphthoquinones (3) were designed and synthesized as new cytotoxic and apoptosis inducing agents by utilizing the anti-parasite drug atovaquone as lead compound. Several compounds displayed significantly improved cytotoxic activities against a panel of cancer cell lines than that of atovaquone. These compounds also induced apoptosis through activating pro-apoptotic caspases 9 and 3.