Design,synthesis and biological evaluation of phenylsulfonamide-based IDO1 inhibitors
10.11665/j.issn.1000 -5048.20180105
- VernacularTitle:苯磺酰胺类IDO1抑制剂的设计、合成和生物活性
- Author:
Shuanglong JIN
1
;
Fang WANG
;
Yi ZOU
;
Yan WANG
;
Yue HU
;
Wenjie GUO
;
Qiang XU
;
Yisheng LAI
Author Information
1. 中国药科大学新药研究中心
- Keywords:
IDO1 inhibitor;
phenylsulfonamide;
synthesis;
biological evaluation
- From:
Journal of China Pharmaceutical University
2018;49(1):34-38
- CountryChina
- Language:Chinese
-
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.
