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

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

Volume: 8 Issue: 4

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

Affiliation:

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

Abstract: 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%.

Cite this article as:

Nam Nguyen-Hai, Anh Ngoc Ngo and Byung Zun Ahn, Synthesis of (6,7-dimethoxy-2-oxo-2H-chromen-4-yl)methyl 3-Arylacrylates as Water Soluble Antitumor Agents, Letters in Drug Design & Discovery 2011; 8 (4) . https://dx.doi.org/10.2174/157018011794839466