Atovaquone derivatives as potent cytotoxic and apoptosis inducing agents

  • Bioorg Med Chem Lett. 2009 Sep 1;19(17):5091-4. doi: 10.1016/j.bmcl.2009.07.044.
Jing Zhou  1 ,  Lei Duan ,  Huaming Chen ,  Xiaomei Ren ,  Zhang Zhang ,  Fengtao Zhou ,  Jinsong Liu ,  Duanqing Pei ,  Ke Ding
Affiliations
  • 1. Key Laboratory of Regenerative Biology, Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, International Business Incubator A-3, Guangzhou Science Park, Guangzhou, China.
PMID: 19632833 DOI: 10.1016/j.bmcl.2009.07.044
Abstract

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.