中国药科大学学报2018，Vol.49Issue(1)：34-38,5.DOI:10.11665/j.issn.1000 -5048.20180105
苯磺酰胺类IDO1抑制剂的设计、合成和生物活性
Design,synthesis and biological evaluation of phenylsulfonamide-based IDO1 inhibitors
摘要
Abstract
Based on the reported IDO1 inhibitor U-3i,11 phenylsulfonamide derivatives were designed and syn-thesized by adopting bioisosterism and molecular docking technology.The inhibitory activities of the target compounds against IDO1 were determined by the HeLa cell-based kynurenine assay.The results demonstrated that most compounds showed different degrees of inhibitory effects on IDO1.Among them,compounds 3b and 3e displayed the most potent activity and could reverse IDO1-mediated immune suppression,which might be worth of further investigation.关键词
IDO1抑制剂/苯磺酰胺/合成/生物活性Key words
IDO1 inhibitor/phenylsulfonamide/synthesis/biological evaluation分类
医药卫生引用本文复制引用
金双龙,王芳,邹毅,王燕,胡月,郭文洁,徐强,赖宜生..苯磺酰胺类IDO1抑制剂的设计、合成和生物活性[J].中国药科大学学报,2018,49(1):34-38,5.基金项目
国家自然科学基金资助项目(No.21472244,No.21472091,No.21772233)This study was supported by the National Natural Science Foundation of China ( No. 21472244, No. 21472091, No. 21772233 （No.21472244,No.21472091,No.21772233）
