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Synthesis and evaluation of mansonone F derivatives as topoisomerase inhibitors

2011; Elsevier BV; Volume: 46; Issue: 8 Linguagem: Inglês

10.1016/j.ejmech.2011.04.059

1768-3254

Wei-Bin Wu, Jie-Bin Ou, Zhihong Huang, Shuo-Bin Chen, Tian‐Miao Ou, Jia‐Heng Tan, Ding Li, Liu‐Lan Shen, Shi‐Liang Huang, Lian‐Quan Gu, Zhi‐Shu Huang,

Synthesis and bioactivity of alkaloids

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.