title: Atovaquone derivatives as potent cytotoxic and apoptosis inducing agents.
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.
authors.affiliation: 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.
authors.forename: Jing
authors.initials: J
authors.lastname: Zhou
authors.forename: Lei
authors.initials: L
authors.lastname: Duan
authors.forename: Huaming
authors.initials: H
authors.lastname: Chen
authors.forename: Xiaomei
authors.initials: X
authors.lastname: Ren
authors.forename: Zhang
authors.initials: Z
authors.lastname: Zhang
authors.forename: Fengtao
authors.initials: F
authors.lastname: Zhou
authors.forename: Jinsong
authors.initials: J
authors.lastname: Liu
authors.forename: Duanqing
authors.initials: D
authors.lastname: Pei
authors.forename: Ke
authors.initials: K
authors.lastname: Ding
mesh_terms: D000890:Anti-Infective Agents / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D017209:Apoptosis; D053626:Atovaquone / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D053148:Caspase 3 / Q000378:metabolism; D053453:Caspase 9 / Q000378:metabolism; D045744:Cell Line, Tumor; D018360:Crystallography, X-Ray; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008297:Male; D008968:Molecular Conformation; D009285:Naphthoquinones / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D011471:Prostatic Neoplasms / Q000188:drug therapy / Q000473:pathology
chemical_list: D000890:Anti-Infective Agents; D000970:Antineoplastic Agents; D009285:Naphthoquinones; D053148:Caspase 3; D053453:Caspase 9; D053626:Atovaquone