Synthesis and evaluation of mansonone F derivatives as topoisomerase inhibitors.

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Wu WB, Ou JB, Huang ZH, Chen SB, Ou TM, Tan JH, Li D, Shen LL, Huang SL, Gu LQ, Huang ZS

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. Epub 2011 May 5.

PubMed ID
21600681 [ View in PubMed
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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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
EtoposideDNA topoisomerase 2-alphaIC 50 (nM)60300N/AN/ADetails