Synthesis and Preliminary Antitumor Activities of Aurone Derivatives

Huang Xinwei; Wang Zheng; Chen Qiaoli; Sun Yanni; Wang Cuiling; Liu Zhulan; Liu Jianli

HERO ID

2830236

Reference Type

Journal Article

Year

2013

HERO ID 2830236
In Press No
Year 2013
Title Synthesis and Preliminary Antitumor Activities of Aurone Derivatives
Authors Huang Xinwei; Wang Zheng; Chen Qiaoli; Sun Yanni; Wang Cuiling; Liu Zhulan; Liu Jianli
Journal Youji Huaxue / Chinese Journal of Organic Chemistry
Volume 33
Issue 12
Page Numbers 2565-2571
Abstract Aurones are an important type of flavonoids with broad biological activities and pharmacological effects, such as anti-tumor, anti-inflammatory, antioxidant, antibacterial, insect antifeedant etc. They are less common and not widely distributed in nature. The low contents in nature lead to high cost of extraction and separation. In order to extend the compounds diversity and study structure activity relationship, phenoxyacetic acid, 2,3,5-trimethylphenol, 4-chlorol-3,5-dimethylphenol, chloroacetic acid and various aromatic aldehydes are used as starting materials to synthesize three types of aurone derivatives. Their structures were characterized by melting point, H-1 NMR, C-13 NMR, ESI-MS and elemental analysis. Nine of twenty five synthetic compounds 2h similar to 2m, 5a similar to 5c were unreported in the literature. All the target compounds were evaluated for antitumor activities against Hela human cervical carcinoma cell lines by methyl thiazolyl tetrazolium (MTT) method. The results showed that compounds 2b, 5b, 2s and 2g exhibited potentially high activity against Hela human cervical carcinoma cell lines with IC50 value of 44.3, 31.1, 43.8 and 41.9 mu mol/L.
Doi 10.6023/cjoc201305032
Wosid WOS:000329686800015
Is Certified Translation No
Dupe Override No
Is Public Yes
Keyword aurone derivatives; synthesis; antitumor activities; structure activity relationship