Synthesis and Evaluation of 4-(4-Hydroxy-3-methoxy benzylidene) curcumin as Potential Hsp90 Inhibitors

Abstract

Abstract: 4-(4-hydroxy-3-methoxyphenyl) methyl curcumin (C085) was synthesized and evaluated for its antitumor activity.C085 was synthesized by Knovenagel condensation. The in vitro antitumor activity of C085 was evaluated by MTT assay against SKBr3,K562,HL-60,HepG2,B-16,SW480,Bxpc-3,SH-SY5Y and MGC80-3 cells. The results showed that C085 inhibited the proliferation of cancer cells (IC₅₀:0.51、1.26、2.90、0.81、1.77、1.31、8.22、1.93、7.41 μmol/L).Western blotting analyses showed that Her2 and AKT degradation were observed upon administration of C085,suggesting this compound exerted activity through Hsp90 inhibition.Molecular docking study also supported C086 as an Hsp90 inhibitor.

Key words: Hsp90, curcumin, 4-arylidene curcumin, antitumor, molecular docking

CLC Number:

R966

LIU Yang1, LI Na2, WU Li-xian3, XU Jian-hua4*. Synthesis and Evaluation of 4-(4-Hydroxy-3-methoxy benzylidene) curcumin as Potential Hsp90 Inhibitors[J]. NATURAL PRODUCT RESEARCH AND DEVELOPMENT, 2014, 26(11): 1729-1732.

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URL: http://www.trcw.ac.cn/EN/

http://www.trcw.ac.cn/EN/Y2014/V26/I11/1729

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Synthesis and Evaluation of 4-(4-Hydroxy-3-methoxy benzylidene) curcumin as Potential Hsp90 Inhibitors

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