4-(N-取代苯基)氨基喹唑啉类化合物的合成及抗磷酸化活性研究

Synthesis and Anti-phosphorylation Activity of 4-Substitutedanilinoquinazoline Compounds

以4-氯喹唑啉为起始原料,经环化、氯化、取代三步反应,合成了8个新的4-取代苯基氨基喹唑啉类化合物.采用1HNMR,13CNMR,MS,IR及元素分析对目标化合物的结构进行了表征.生物活性测试表明,化合物1f在1μmol?L-1浓度下对PC3细胞增殖抑制活性达到88.6%,进一步研究表明该化合物具有较高的抑制细胞外信号调节激酶(ERK)磷酸化的活性.

Eight new 4-substitutedquinazoline compounds were synthesized by three-step reaction using 4-chloroquinazoline as starting material. The structures of the title compounds were characterized by elemental analyses, IR, ^1H NMR, ^13C NMR and MS spectra. The results of bioassay showed that compound If had good antiproliferation activity against cancer cell PC3 with rate of 88.6% at the concentration of 1μmol·L^-1 and inhibits ERK （extracellular signal-regulated kinase） phosphorylation in cells PC3 induced by EGFR （epidermal growth factor receptor）.