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

被引：2

作者：

Nguyen-Hai Nam ^{[1
]}

Ngo Anh Ngoc ^{[2
]}

Zun, Ahn Byung ^{[3
]}

机构：

[1] Hanoi Univ Pharm, Dept Pharmaceut Chem, Hanoi, Vietnam

[2] Univ Paris 11, Paris, France

[3] Chungnam Natl Univ, Taejon, South Korea

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2011年 / 8卷 / 04期

关键词：

Coumarin; Cytotoxicity; Water solubility; Antitumor activity; DERIVATIVES; CELLS;

D O I：

10.2174/157018011794839466

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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%.

引用

页码：312 / 316

页数：5

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