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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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 and Ahn Byung Zun

Volume 8, Issue 4, 2011

Page: [312 - 316] Pages: 5

DOI: 10.2174/157018011794839466

Price: $65

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%.

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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