Anticancer Evaluation of 3,4,5,4'-trans-tetramethoxystilbene (DMU-212) and Its Analogs Against an Extensive Panel of Human Tumor Cell Lines

DMU-212, a methoxylated resveratrol analog, has significant anticancer activity, and selectively targets tumor cells. A library of E-diarylstilbenes structurally related to DMU-212 has been synthesized and evaluated for anticancer activity against a large panel of 45 human cancer cell lines. From this study, DMU-212 (3a) exhibited an average growth inhibitory effect (GI50) of 3.5 μM against all the human cancer cell lines in the panel, and was particularly effective against the four cancer cell lines: SNB-75 (CNS), MDA-MB-435 (melanoma), A498 (renal), and MCF7 (breast), with GI50 values of 1.88, 1.04, 0.74 and 1.66 μM, respectively. Also, the 4’-chloro analog of DMU-212, 3d, exhibited 98 and 80 percent growth inhibition against MDA-MB-435 (melanoma) and K-562 (leukemia) cancer cell lines at a concentration of 10 μM. Further investigation of DMU-212 and its analogs may provide novel therapeutic avenues for treatment of a variety of human cancers.