摘要
经2-氨基-5-氟苯甲酸与甲酰胺闭环、氯化反应,合成了6-氟-4-氯喹唑啉,然后在微波辐射下与芳香胺反应,合成了6个新的6-氟-4-(N-芳基)胺基喹唑啉类化合物.新化合物经1HNMR,IR及元素分析证明其结构.体外抑瘤试验证明化合物对前列腺癌细胞(PC3)、人胃癌细胞(BGC823)、人乳腺癌细胞(BCap-37)均无抑制活性.经ERK的抗磷酸化活性免疫印迹试验证明化合物对小鼠成纤维细胞(NIH3T3)无抑制活性.
Six new 6-fluoro-4-（N-aryl）aminoquinazoline compounds were synthesized, firstly by the cyclization reaction of 2-amino-5-fluorobenzoic acid with formamide and then chlorination to attain 4-chloro-6-fluoroquinazoline, finally the amination with arylamines under microwave irradiation. The structures of the six new compounds were characterized by elemental analyses, IR and ^1H NMR spectra. Bioactivity of the new compounds was tested. The results showed that the six new compounds had weak anticancer activity to PC3, BGC823, BCap-37 and ERK phosphorylation in NIH3T3 cell induced by PDGF.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2006年第9期1275-1278,共4页
Chinese Journal of Organic Chemistry
基金
国家自然科学基金(No.20562003)
2005年贵州省优秀青年科技人才(No.20050515)资助项目.
关键词
喹唑啉
氟
合成
微波辐射
生物活性
qunazoline
fluorine
synthesis
microwave irradiation
bloactlvlty
作者简介
E-mail： songbaoan22@yahoo.com; Fax： 0851-3622211.
