高等学校化学学报2017，Vol.38Issue(9)：1590-1595,6.DOI:10.7503/cjcu20170136
PI3 K/mTOR抑制剂的合成及生物活性
Synthesis and Biological Activity of Novel PI3K/mTOR Inhibitors
摘要
Abstract
A series of new phosphatidylinositol 3-kinase/mammalian target of rapamycin ( PI3K/mTOR ) inhibitors with optimized synthetic process was designed and synthesized, the correctness of the structure was determined by 1 H NMR and LC-MS and the antitumor activities of these compounds were evaluated in 3 tumor celllines by MTT colorimetric method. Compound 11 showed very strong inhibition of MV4-11 cell growth, and was selected as a leading compound for further development of anti-leukemia drug candidate.关键词
磷脂酰肌醇3-激酶/哺乳动物雷帕霉素靶蛋白抑制剂/抗肿瘤活性/构效关系Key words
Phosphatidylinositol 3-kinase/mammalian target of rapamycin( PI3K/mTOR) inhibitor/Antitumor viability/Structure-activity relationship分类
化学化工引用本文复制引用
王磊,郑国钧,季奇,陈博,巩龙龙,高聪敏,杜镇建,张兴民..PI3 K/mTOR抑制剂的合成及生物活性[J].高等学校化学学报,2017,38(9):1590-1595,6.基金项目
北京市科委生物医药创新品种研发项目(批准号: Z161100000116018)和北京市经济技术开发区科技创新专项项目(批准号:JSYF2013138)资助. Supported by the Research and Development Project of Beijing Municipal Commission of Science and Technology, China ( No. Z161100000116018) and the Science & Technology Innovation of Beijing Economic-Technological Development Area, China(No.JSYF2013138). （批准号: Z161100000116018）
