Synthesis of (6,7-dimethoxy-2-oxo-2H-chromen-4-yl)methyl 3-Arylacrylates as Water Soluble Antitumor Agents

Author(s): Nguyen-Hai Nam, Ngo Anh Ngoc, Ahn Byung Zun

Journal Name: Letters in Drug Design & Discovery

Volume 8 , Issue 4 , 2011

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Four (6,7-dimethoxy-2-oxo-2H-chromen-4-yl)methyl 3-arylacrylate (5a-d) analogues of the antitumor agent (6,7-dimethoxy-2-oxo-2H-chromen-4-yl)methyl 3-(4-methoxyphenyl)acrylate (2) were synthesized. The compounds 5a-d have one or two nitrogen atoms incorporated on the aryl moiety, and therefore could be converted into hydrochloride salts (6a-d) and these salts possess greater water solubility compared to 2. Antitumor activity evaluation of using BDF1 mice bearing 3LL tumor cells model demonstrated significant inhibitory effects of compounds 6a-d against tumor growth with inhibition rates from 37.2 to 48.2%.

Keywords: Coumarin, Cytotoxicity, Water solubility, Antitumor activity, Antimicrobial, Antifungal, Human immunodeficiency Virus (HIV), Umbilical Venous, Endothelial Cells, Cancer Cell Lines, Analogues, Cinnamoyl Moiety, Tumor Cells, Bovine Serum

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Article Details

Year: 2011
Page: [312 - 316]
Pages: 5
DOI: 10.2174/157018011794839466
Price: $65

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