Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin
Synthesis and evaluation of a series of resveratrol analogues as potent anti-cancer agents that target tubulin
Nikhil R. Madadi,1 Hongliang Zong,2 Amit Ketkar,3 Chen Zheng,1 Narsimha R. Penthala,1 Venumadhav Janganati,1 Shobanbabu Bommagani,1 Robert L. Eoff,3 Monica L. Guzman,2 and Peter A. Crooks1,*
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1 Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA
2 Division of Hematology and Medical Oncology, Department of Medicine, Weill Medical College of Cornell University, New York, NY
3 Department of Biochemistry and Molecular Biology, College of Medicine, University of Arkansas for Medical Sciences, Little Rock, AR 72205, USA
Abstract
A series of novel diarylacrylonitrile and trans-stilbene analogues of resveratrol has been synthesized and evaluated for their anticancer activities against a panel of 60 human cancer cell lines. The diarylacrylonitrile analogues 3b and 4a exhibited the most potent anticancer activity of all the analogues synthesized in this study, with GI50 values of < 10 nM against almost all the cell lines in the human cancer cell panel. Compounds 3b and 4a were also screened against the acute myeloid leukemia (AML) cell line, MV4-11, and were found to have potent cytotoxic properties that are likely mediated through inhibition of tubulin polymerization.