Novel 5-Methyl-2,4-Disubstitued-Oxazole Derivatives: Synthesis and Anticancer Activity

被引：3

作者：

Liu, Xin-Hua ^{[1
,2
]}

Liu, Hui-Feng ^{[2
]}

Pan, Chun-Xiou ^{[2
]}

Liu, Jin-Xin ^{[2
]}

Bai, Lin-Shan ^{[2
]}

Song, Bao-An ^{[1
]}

Chu, Xiang-Feng ^{[2
]}

机构：

[1] Guizhou Univ, Key Lab Green Pesticide & Agr Bioengn, Minist Educ, Guiyang 55002, Peoples R China

[2] Anhui Univ Technol, Sch Chem & Chem Engn, Maanshan 243002, Peoples R China

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2010年 / 7卷 / 04期

基金：

中国国家自然科学基金;

关键词：

Oxazole; Quoline; Synthese; Pyrazine; Antitumor activity; INHIBITORS; FLUORINE; BIOACTIVITY; CHEMISTRY; OXAZOLES; PROTEIN; ANALOG;

D O I：

10.2174/157018010790945878

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 5-methyl-2,4-disubstitued-oxazole derivatives were synthesized and evaluated for their antitumor activities. The bioassay tests showed that 7-(5-methyl-2-(4-(R)phenyl)oxazol-4-yl)quinoline (R = trifluoromethyl, 2a; fluoro, 2b; chloro) and 2-(5-methyl-2-(4-(trifluoromethyl or fluoro) phenyl)oxazol-4-yl) pyrazine derivatives (4a and 4b) were highly effective against PC-3 cell with the IC50 values ranging from 1.2 to 2.0 mu g/mL. 2-(2-(2,4-dichlorophenyl or 2,4-difluoro phenyl)-5-methyloxazol-4-yl)pyrazine (4e and 4f) were highly effective against A431 cell. The IC50 values of 4e and 4f against A431 cell were 2.0 and 1.6 mu g/mL, respectively.

引用

页码：238 / 243

页数：6

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