Atovaquone derivatives as potent cytotoxic and apoptosis inducing agents.
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.
Zhou
Jing
J
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.
Duan
Lei
L
Chen
Huaming
H
Ren
Xiaomei
X
Zhang
Zhang
Z
Zhou
Fengtao
F
Liu
Jinsong
J
Pei
Duanqing
D
Ding
Ke
K
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
D000890:Anti-Infective Agents; D000970:Antineoplastic Agents; D009285:Naphthoquinones; D053148:Caspase 3; D053453:Caspase 9; D053626:Atovaquone