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United States Department of Agriculture

Agricultural Research Service

Title: In vitro and In vivo Studies on Stilbene Analogs as Potential Treatment Agents for Colon Cancer)

Author
item Paul, Shiby
item Mizuno, Cassia
item Lee, Hong Jin
item Zheng, Xi
item Chajkowisk, Sarah
item Rimoldi, John
item Conney, Allan
item Suh, Nanjoo
item Rimando, Agnes

Submitted to: European Journal of Medicinal Chemistry
Publication Type: Peer Reviewed Journal
Publication Acceptance Date: 5/8/2010
Publication Date: 5/15/2010
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.

Technical Abstract: 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.

Last Modified: 8/24/2016
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