摘要
以6-碘喹唑啉-4-酮为原料,经氯代、胺化、Suzuki偶联、Wittig-horner等反应合成了7个新型的4-取代苯胺喹唑啉衍生物(5a^5g),其结构经1H NMR和HR-MS(ESI)表征。采用MTT法研究了5a^5g对人乳腺癌细胞(MCF-7)、人肺癌细胞(A549)和人皮肤鳞癌细胞(A431)的抑制活性。结果表明:5a^5g对肿瘤细胞均具有明显的抑制活性;其中5e的抑制活性(IC50=0.13~5.26μmol·L-1)优于拉帕替尼(IC50=0.21~15.56μmol·L-1)。
Seven novel 4-substituted anilinoquinazoline derivatives（ 5 a ～ 5 g） were synthesized from 6-iodoquinazolin-4-one by chlorination,amination,Suzuki coupling and Wittig-Horner reaction. The structures were characterized by1 H NMR and HR-MS（ ESI）. The in vitro antitumor activities of 5 a ～5 g against human cancer cells A-549,MCF-7 and A431 were investigated by MTT method. The results indicated that 5 a ～ 5 g showed good inhibition activities and 5 e showed better inhibition activities（ IC50= 0. 13 ～ 5. 26 μmol·L～（-1）） than Lapatinib（ IC50= 0. 21 ～ 15. 56 μmol·L～（-1））.
作者
金正盛
蔡志强
方舒慧
赵蓉
丁海关
曹慧
许娣
孟苗苗
李英杰
马启朋
JIN Zheng-sheng;CAI Zhi-qiang;FANG Shu-hui;ZHAO Rong;DING Hai-guan;CAO Hui;XU Di;MENG Miao-miao;LI Ying-jie;MA Qi-peng(School of Petrochemical Engineering,Shenyang University of Technolog,Liaoyang 111003,China;Key Laboratory for Chemical Drug Research of Shandong Province,Institute of Phamaceutical Sciences of Shandong Province,Jinan 250101,China;Petrochina,Fushun Petrochemical Company,Fushun 113008,China)
出处
《合成化学》
CAS
CSCD
北大核心
2018年第6期389-393,399,共6页
Chinese Journal of Synthetic Chemistry
基金
辽宁省教育厅科学研究项目(L2015383)
博士科研启动基金(521422)
沈阳市科技计划项目(18-004-4-32)
