新型芳基脲类血管内皮生长因子受体抑制剂的合成与抗肿瘤活性研究  

Synthesis and Antitumor Activity of Novel Aryl Urea Derivatives as Vascular Endothelial Growth Factor Receptor Inhibitors

作　　者：余杨潇 赵砚瑾[2] 常先磊 于清华[2] 张志杰[2] 罗鸣锐 李庶心[1,2] 

机构地区：[1]广西医科大学,广西南宁530021 [2]军事医学科学院放射与辐射医学研究所,北京100850 [3]武汉工程大学,湖北武汉430205

出　　处：《解放军药学学报》2016年第3期198-201,共4页Pharmaceutical Journal of Chinese People's Liberation Army

基　　金："重大新药创制"国家科技重大专项;No.2012ZX09102101-013

摘　　要：目的合成新型芳基脲类血管内皮生长因子受体抑制剂并评价其抗肿瘤活性。方法以Tivozanib为先导化合物进行结构改造,设计合成系列芳基脲类衍生物,1H-NMR和ESI-MS鉴定目标物结构,并用MTT法进行体外抑制肿瘤细胞增殖活性评价。结果合成10个新目标化合物,其中7个表现出显著的体外抑制肿瘤细胞增殖活性。结论目标化合物体外活性好,值得进一步研究。Objective To synthesize novel aryl urea antitumor agents and conduct a preliminary investigation on their activity. Methods With tivozanib as the lead compound, ten novel aryl urea compounds were designed, synthesized and characterized by 1H-NMR and ESI-MS. Their antitumor activities were screened by MTT methods. Resuits Ten novel compounds were synthesized, seven of which had better antitumor activities in vitro than tivozanib. Conclusion The target compounds have remarkable antitumor activities in vitro , which are worthy of further studies.

关 键 词：抗肿瘤药 VEGFR抑制剂 芳基脲衍生物 

分 类 号：R915.5[医药卫生—微生物与生化药学]