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苯磺酰胺类IDO1抑制剂的设计、合成和生物活性评价
投稿时间:2017-05-16  修订日期:2017-05-18  点此下载全文
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作者单位E-mail
王芳 中国药科大学 924729644@qq.com 
邹毅 中国药科大学 zycz138@163.com 
王燕 南京大学  
郭文杰 南京大学  
徐强 南京大学  
赖宜生 中国药科大学 yslai@cpu.edu.cn 
基金项目:国家自然科学基金项目(面上项目,重点项目,重大项目)
中文摘要:在IDO1抑制剂U-3i的基础上,利用生物电子等排原理,结合分子对接技术,设计并合成了11个苯磺酰胺类目标化合物。采用基于HeLa细胞酶学测定方法评价了目标化合物对IDO1的抑制活性。结果表明,大多数化合物对IDO1显现出不同程度的抑制,其中,化合物3b和3e的抑制活性最强,而且两者能够有效逆转IDO1介导的免疫逃逸,值得进一步研究。
中文关键词:IDO1抑制剂  苯磺酰胺  合成  生物活性评价
 
Design, synthesis and biological evaluation of phenylsulfonamide-based IDO1
Abstract:Based on the reported IDO1 inhibitor U-3i, we designed and synthesized 11 phenylsulfonamide derivatives 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 the target compounds showed different inhibitory effects on IDO1. Among them, 3b and 3e displayed the most potent activity and could reverse IDO1-mediated immune suppression, suggesting that these compounds might be the candidates for further investigation.
keywords:IDO1 inhibitor  phenylsulfonamide  synthesis  biological evaluation
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