CHEMISTRY OF NATURAL PRODUCTS FOR PEST MANAGEMENT AND CROP DEVELOPMENT
Location: Natural Products Utilization Research
Title: In vitro and In vivo Studies on Stilbene Analogs as Potential Treatment Agents for Colon Cancer
| Paul, Shiby - |
| Mizuno, Cassia |
| Lee, Hong Jin - |
| Zheng, XI - |
| Chajkowisk, Sarah - |
| Rimoldi, John - |
| Conney, Allan - |
| Suh, Nanjoo - |
Submitted to: European Journal of Medicinal Chemistry
Publication Type: Peer Reviewed Journal
Publication Acceptance Date: May 8, 2010
Publication Date: May 15, 2010
Citation: Paul, S., Mizuno, C.S., Lee, H., Zheng, X., Chajkowisk, S., Rimoldi, J.M., Conney, A., Suh, N., Rimando, A.M. 2010. In vitro and In vivo Studies on Stilbene Analogs as Potential Treatment Agents for Colon Cancer. European Journal of Medicinal Chemistry. 45:3702-3708.
Interpretive Summary: Colon cancer is the third most common type of cancer found in the United States. Resveratrol, a natural compound found in grapes has shown to have anticancer activities. For this reason a number of resveratrol like compounds were made and tested against colon cancer cells and in rats. Two compounds were identified as having very good anticancer activity. This work is a contribution towards the advancement in the treatment of colon cancer using natural based compounds.
Based upon the potential of resveratrol as a cancer chemopreventive agent, 27 stilbenes analogs were synthesized and tested against colon cancer cell line HT-29. Among these compounds, amino derivative (Z)-4-(3,5-dimethoxystyryl) aniline (4), (Z)-methyl 4-(3,5-dimethoxystyryl) benzoate (6) and (Z)-1,3-dimethoxy-5-(4-methoxystyryl) benzene (10) showed activities in the low micromolar range. In vivo studies on 4, 6 and 10, and on their corresponding trans isomers 3, 5 and 9, respectively, using HT-29 xenografts in immunodeficient mice revealed that cis and trans amino analogs 3 and 4 decreased tumor growth by 40% compared to controls.