title: Synthesis and evaluation of mansonone F derivatives as topoisomerase inhibitors.
abstract: A series of mansonone F (MF) derivatives were designed and synthesized. These compounds were found to be strong inhibitors for topoisomerases, with much more significant inhibition for topoisomerase II rather than topoisomerase I. The best inhibitor showed 20 times stronger anti-topoisomerase II activity than a positive control Etoposide. The cytotoxic activity of these MF derivatives was evaluated against human cancer cell lines CNE-2 and Glc-82, which showed that these compounds were potent antitumor agents. The structure-activity relationships (SARs) study revealed that o-quinone group and pyran ring are important for their cytotoxic activity.
authors: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou University City, Waihuan East Road 132, Guangzhou 510006, People's Republic of China.
authors: Wei-Bin
authors: WB
authors: Wu
authors: Jie-Bin
authors: JB
authors: Ou
authors: Zhi-Hong
authors: ZH
authors: Huang
authors: Shuo-Bin
authors: SB
authors: Chen
authors: Tian-Miao
authors: TM
authors: Ou
authors: Jia-Heng
authors: JH
authors: Tan
authors: Ding
authors: D
authors: Li
authors: Liu-Lan
authors: LL
authors: Shen
authors: Shi-Liang
authors: SL
authors: Huang
authors: Lian-Quan
authors: LQ
authors: Gu
authors: Zhi-Shu
authors: ZS
authors: Huang