高等学校化学学报Issue(5)：981-988,8.DOI:10.7503/cjcu20130837
新型含缩氨基硫脲结构的喹唑啉衍生物的合成及体外抗癌活性
Synthesis and In vitro Anticancer Activity of Novel Quinazoline Derivatives Containing Thiosemicarbazone Structure
摘要
Abstract
To find new EGFR inhibitors, 15 novel quinazoline derivatives containing thiosemicarbazone struc-ture were designed and synthesized from 2-amino-4 ,5-dimethoxybenzoic acid and formamidine acetate by the cyclization, chlorination, amination and condensation reactions. All structures of target compounds were con-firmed by 1 H NMR,13 C NMR, HRMS and elemental analysis. The in vitro anticancer activities of compounds 6a—6o against EGFR over-expressing of MCF-7(Human breast cancer), A549(Human pulmonary adenocar-cinoma) and PC3(Human prostate cancer) cell lines were tested using colorimetric MTT assay. The results indicated that several compounds showed potent activity. Compounds 6a and 6o were more potent than Lapa-tinib, but slightly weaker than ADM against the three cell lines. The IC50 values of compounds 6a and 6o against MCF-7 cell line were 6. 97 and 6. 99 μmol/L, against A549 were 5. 15 and 3. 11 μmol/L and against PC3 were 2. 30 and 1. 42μmol/L, respectively. Preliminary structure-activity relationship was also discussed.关键词
表皮生长因子受体( EGFR)/喹唑啉/缩氨基硫脲/抗癌活性Key words
Epidermal growth factor receptor( EGFR)/Quinazoline/Thiosemicarbazone/Anticancer activity分类
化学化工引用本文复制引用
刘海彬,吕萍,潘宁宁,艾丽梅,刘永祥..新型含缩氨基硫脲结构的喹唑啉衍生物的合成及体外抗癌活性[J].高等学校化学学报,2014,(5):981-988,8.基金项目
辽宁省高等学校优秀人才支持计划(批准号:LJQ2011130)、国家自然科学基金(批准号:21202103)和辽宁省教育厅科研项目(批准号:L2010204)资助.覮Supported by the Program for Liaoning Excellent Talents in University(No. LJQ2011130), the National Natural Science Foundation of China (No.21202103) and the Program of Liaoning Provincial Committee of Education, China(No. L2010204) （批准号:LJQ2011130）
