Design, synthesis, and evaluation of methoxylated resveratrol derivatives as potential antitumor agents.

Resveratrol (3,5,4′-trihydroxystilbene), a naturally occurring stilbene that occurs in a variety of foods and beverages, has attracted increasing attention over the past decade because of its beneficial bioactivity, including chemopreventive and antitumor activity. Because several resveratrol derivatives are structurally similar to resveratrol, a set of 26 methoxylated trans-stilbene resveratrol derivatives were synthesized and evaluated for their in-vitro antitumor activity against three cancer cell lines (K562, HT29, and HePG2). Pharmacological data indicated that several of the derivatives had marked antiproliferative activity compared with resveratrol, as reference, especially the most promising compound (IC values 1.28, 0.59 and 0.98 μM against K562, HT29, and HePG2 cell lines, respectively). Substitution of the stilbene structure with methoxy at the C-4′ position had the greatest effect on activity. The anti-tumor potential of these compounds could serve as a basis for development of novel antitumor agents. [ABSTRACT FROM AUTHOR]