摘要
为了寻求高效的新型抗肿瘤药物,设计并合成了一系列新型2-甲硫基-4-苯胺喹唑啉衍生物,对这些化合物在人类四种癌细胞MGC-803(人胃癌细胞)、PC-3(人前列腺癌细胞)、HGC-27(人胃癌细胞)和A549(人非小细胞肺癌细胞)进行抗肿瘤活性评价.结果显示部分化合物具有较好的抗肿瘤活性,其中N-(4-氟苯基)-2-(甲硫基)喹唑啉-4-胺(9c)和N-(4-甲基苯基)-2-(甲硫基)喹唑啉-4-胺(9m)显示出较高的抗肿瘤活性, IC_(50)值分别为0.18和0.68μmol·L^(-1).
In order to find the efficient and novel antitumor drugs,a series of 2-methylthio-4-arylamine quinazoline derivatives were designed and synthesized.The target compounds were evaluated for antitumor activity in vitro on four human cancer cell lines initially including MGC-803,PC-3,HGC-27 and A549.The results showed that some compounds had good antitumor activities,especially N-(4-fluorophenyl)-2-(methylthio)quinazolin-4-amine(9c) and 2-(methylthio)-N-(p-tolyl)-quina-zolin-4-amine(9 m),with IC50 values of 0.18 and 0.68 μmol·L-1,respectively.
作者
孟祥川
栗娜
李二冬
常通航
刘梦
柳晴怡
袁文娟
张晴晴
张钰
周智玉
宋攀攀
刘宏民
张秋荣
Meng Xiangchuan;Li Na;Liu Qingyia;Yuan Wenjuana;Song Panpan;Li Erdong;Chang Tonghang;Zhang Qingqing;Liu Hongmin;Zhang Yua;Zhang Qiurong;Liu Menga;Zhou Zhiyu(School of Pharmaceutical Science,Zhengzhou University,Zhengzhou 450001;Collaborative Innovation Center of New Drug Research and Safety Evaluation,Zhengzhou 450001)
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2018年第11期3063-3069,共7页
Chinese Journal of Organic Chemistry
基金
国家自然科学基金(No.81430085)
河南省科技厅项目(Nos.182300410321
182102310249)
郑州大学大学生创新创业训练计划(No.2017cxcy563)资助项目~~
关键词
喹唑啉衍生物
合成
抗肿瘤活性
评价
quinazoline derivatives
synthesis
antitumor activity
evaluation
