高等学校化学学报Issue(12)：2584-2592,9.DOI:10.7503/cjcu20140333
吡啶联异唑类化合物的设计、合成及抗肿瘤活性
Design and Synthesis of Pyridinylisoxazoles and Their Anticancer Activities
摘要
Abstract
Based on the X-ray co-crystal structures of reported allosteric kinase inhibitors bound to their corresponding protein kinases, a pharmacophore model was proposed. To examine the validity of this hypothe-sis, 21 new pyridinylisoxazole derivatives were designed and synthesized. Their structures were confirmed using 1 H NMR, 13 C NMR and MS data. Their inhibitory effects against human breast cancer cell ( MCF-7 ) proliferation were evaluated. Preliminary results indicated that some of these pyridinylisoxazole derivatives possess potent anti-proliferative activities, with IC50 data in the micromolar range. The mechanism-of-action of these compounds is under investigation.关键词
吡啶联异唑/蛋白激酶/变构抑制剂/抗肿瘤活性Key words
Pyridinylisoxazole/Protein kinase/Allosteric kinase inhibitor/Antitumor activity分类
化学化工引用本文复制引用
杨洪亮,徐国兴,宝梅英,张大鹏,李志伟,裴亚中..吡啶联异唑类化合物的设计、合成及抗肿瘤活性[J].高等学校化学学报,2014,(12):2584-2592,9.基金项目
国家自然科学基金(批准号:81172914,81071743)、吉林大学唐敖庆教授启动资金和吉林省人才开发基金(批准号:802110000432)资助.覮Supported by the National Natural Science Foundation of China(Nos.81172914,81071743), the Tang Aoqing Professorship Research Grant from Jilin University, China and Jilin Province Talent Development Program, China(No.802110000432) （批准号:81172914,81071743）
