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

Authors: PAUL, SHIBY - Rutgers University; Mizuno, Cassia; LEE, HONG JIN - Rutgers University; ZHENG, XI - Rutgers University; CHAJKOWISK, SARAH - University Of Mississippi; RIMOLDI, JOHN - University Of Mississippi; CONNEY, ALLAN - Rutgers University; SUH, NANJOO - Rutgers University; 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.