AEI 88 |
| Topoisomerase II is a validated anti-cancer target for the treatment of thirteen cancers including small cell lung cancer and many lymphomas. Current topoisomerase II inhibitors act by stabilizing the DNA-topoisomerase II complex, interrupting DNA synthesis and inducing cell death. Simocyclinone D8 is a natural product that has been shown to inhibit topoisomerase II by a new mechanism of action. It is as potent as the front line therapies etoposide and doxorubicin, to which many tumors are becoming resistant. In order to determine the molecular basis for this novel mechanism of action, we are exploring the medicinal chemistry of simocyclinone D8. The natural product has been produced by fermentation from the bacteria S. antibioticus Tu6040, isolated, and purified. Preliminary studies into the absolute structure of simocyclinone D8 and the preparation of derivatives by semi- and total synthesis to probe the structure-activity relationship of this new topoisomerase inhibitor will be reported.
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Academic Employment Initiative
8:00 PM-10:00 PM, Monday, August 20, 2007 BCEC -- Exhibit Hall - B2, Sci-Mix
Academic Employment Initiative |
