Discovery of Novel Tricyclic 5H-Pyridazino[4,5-b]indoles as Potent Antitumor Agents： Design, Synthesis and Biological Evaluation
Discovery of Novel Tricyclic 5H-Pyridazino[4,5-b]indoles as Potent Antitumor Agents： Design, Synthesis and Biological Evaluation作者机构：Key Laboratory of Structure-based Drug Design and Discovery Ministry of EducationShenyang Pharmaceutical University Shenyang 110016 P.R.China
出 版 物：《Chemical Research in Chinese Universities》 (高等学校化学研究（英文版）)
年 卷 期：2015年第31卷第3期
页 面：372-380页
核心收录：
学科分类：1007[医学-药学(可授医学、理学学位)] 083002[工学-环境工程] 100705[医学-微生物与生化药学] 0830[工学-环境科学与工程（可授工学、理学、农学学位）] 07[理学] 08[工学] 0713[理学-生态学] 10[医学]
基 金：the National Natural Science Foundation of China(No.81273357)and the Liaoning Baiqianwan Talents Pro- gram China(No.2013921042)
主 题：1-Anilino-5H-pyridazino[4,5-b]indole EGFR inhibitor Cytotoxicity
摘 要：A novel series of 5H-pyridazino[4,5-b]indoles（L-01-L-32） was synthesized and characterized by means of 1H NMR, MS and elemental analysis. The cytotoxicity of the target compounds against Bel-7402 and HT-1080 cell lines were evaluated by 3-（4,5-dimethylthiazol-2-y1）-2,5-diphenyltetrazolium bromide（MTT） assay. Most of them exhibited moderate to excellent cytotoxicity, and six compounds（L-04, L-06, L-18, L-20, L-21 and L-23） possessed dramatically increased cytotoxicity superior to Gefitinib. Of these initial hits, compound L-21 displayed remarkable cytotoxicity against the tested cell lines with half maximal inhibitory concentration（IC50） values of 4.6 and 2.1 μmol/L, respectively, which was 13.9- to 25.6-fold more potent than positive control.
维普期刊数据库