2. Academic Validation
  3. Synthesis and evaluation of mansonone F derivatives as topoisomerase inhibitors

Synthesis and evaluation of mansonone F derivatives as topoisomerase inhibitors

  • Eur J Med Chem. 2011 Aug;46(8):3339-47. doi: 10.1016/j.ejmech.2011.04.059.
Wei-Bin Wu 1,  Jie-Bin Ou,  Zhi-Hong Huang,  Shuo-Bin Chen,  Tian-Miao Ou,  Jia-Heng Tan,  Ding Li,  Liu-Lan Shen,  Shi-Liang Huang,  Lian-Quan Gu,  Zhi-Shu Huang
Affiliations

Affiliation

  • 1 School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou University City, Waihuan East Road 132, Guangzhou 510006, People's Republic of China.
PMID: 21600681 DOI: 10.1016/j.ejmech.2011.04.059
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.

Figures