Identification of a Novel Indoleamine 2,3-Dioxygenase Inhibitor Bearing an Eight-Membered Ring Fused Indole Scaffold and Its Structure-Activity Relationship
- 1 January 2021
- journal article
- research article
- Published by The Japan Institute of Heterocyclic Chemistry in HETEROCYCLES
- Vol. 103 (1), 331-347
- https://doi.org/10.3987/com-20-s(k)17
Abstract
Indoleamine 2,3-dioxygenase 1 (IDO1) is a promising target for cancer immunotherapy because it is overexpressed in a variety of tumor cells. IDO1 also plays an important role in the process of immune escape by tumors. In this study, we identified a novel IDO1 inhibitor KPYC12532 (5a) bearing an eight-membered ring-fused indole scaffold by screening our compound library. To develop novel IDO1 inhibitors, we conducted a structure-activity relationship study of 5a and found some compounds displaying comparable activity. These results provide useful insight for the design of novel IDO1 inhibitors.Keywords
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