Synthesis and antiproliferative activity of curcumin analogs

MEDI 111

James R. Fuchs, fuchs.42@osu.edu1, Jonathan P. Etter1, Pui-Kai Li1, Dalia Abdelhamid1, Nicholas Regan1, Deepak Bhasin1, Bulbul Pandit1, Chenglong Li1, Katryna Cisek1, Jiayuh Lin2, Ling Cen2, and Brian Hutzen2. (1) Division of Medicinal Chemistry and Pharmacognosy, The Ohio State University, College of Pharmacy, Riffe Building, 496 W. 12th Ave., Columbus, OH 43210, (2) Center for Childhood Cancer, Columbus Children's Research Institute, The Ohio State University, Columbus, OH 43205
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.

 

General Poster Session
7:00 PM-9:00 PM, Sunday, August 17, 2008 Pennsylvania Convention Center -- Hall C, Poster

Division of Medicinal Chemistry

The 236th ACS National Meeting, Philadelphia, PA, August 17-21, 2008