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

作者：Madadi Nikhil Reddy; Crooks Peter Anthony^*

来源：Letters in Drug Design and Discovery, 2015, 12(7): 521-528.

DOI：10.2174/1570180812999150324163710

• Resveratrol
• DMU-212
• anticancer
• growth inhibition
• cytotoxicity
• diarylstilbenes

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 (GI(50)) of 3.5 mu M 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 GI(50) values of 1.88, 1.04, 0.74 and 1.66 mu M, 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 mu M. Further investigation of DMU-212 and its analogs may provide novel therapeutic avenues for treatment of a variety of human cancers.

• 出版日期2015