Authors:
James R. Fuchs, Jonathan P. Etter, Pui-Kai Li, Dalia Abdelhamid, Nicholas Regan, Deepak Bhasin, Bulbul Pandit, Chenglong Li, Katryna Cisek, Jiayuh Lin, Ling Cen, and Brian Hutzen
Summary:
Curcumin, a natural product isolated from the rhizome of Curcuma longa, has been shown to have useful antioxidant, anti-inflammatory, antiangiogenic, and antiproliferative properties due to its interaction with numerous biological targets. Although not as potent as many other cytotoxic agents, curcumin has been demonstrated to be safe in humans at relatively high doses (10 grams/day), making it an attractive target for chemotherapeutic drug discovery efforts. Unfortunately, however, it also suffers from poor bioavailability and stability issues. Therefore, the design and preparation of more potent, stable, and target-selective curcumin analogues is highly desirable. A thorough study of analogues designed to probe both steric and electronic requirements for anticancer activity in breast, colon, and prostate cancer cells is ongoing. Accordingly, our synthetic efforts to prepare these compounds and an investigation into their affected molecular targets will be reported.
Source:
The 236th American Chemical Society National Meeting; Philadelphia, PA, Hall C, Poster, 7:00 PM-9:00 PM (08/17/08)