Design and synthesis of dimethylaminomethyl-substituted curcumin derivatives/analogues: Potent antitumor and antioxidant activity, improved stability and aqueous solubility compared with curcumin

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• 作者：Xubin Fang^a ; ^b ; ^&dagger ; ; Lei Fang^a ; ^b ; ^c ; ^&dagger ; ; ^{lei.fang@seu.edu.cn} ; Shaohua Gou^a ; ^b ; ^{sgou@seu.edu.cn} ; Lin Cheng^a ; ^b
• 关键词：SAR ; structure&ndash ; activity relationship ; DPPH ; 2 ; 2-diphenyl-1-picrylhydrazyl ; FRSA ; free radical scavenging activity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2013
• 出版时间：1 March, 2013
• 年：2013
• 卷：23
• 期：5
• 页码：1297-1301
• 全文大小：653 K

文摘

A series of dimethylaminomethyl-substituted curcumin derivatives/analogues were designed and synthesized. All compounds effectively inhibited HepG2, SGC-7901, A549 and HCT-116 tumor cell lines proliferation in MTT assay. Particularly, compounds 2a and 3d showed much better activity than curcumin against all of the four tumor cell lines. Antioxidant test revealed that these compounds had higher free radical scavenging activity than curcumin towards both DPPH and galvinoxyl radicals. Furthermore, the aqueous solubility and stability of the target compounds were also significantly improved compared with curcumin.