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Paper | Special issue | Vol 103, No. 1, 2021, pp.331-347
Published online, 29th July, 2020
DOI: 10.3987/COM-20-S(K)17
■ Identification of a Novel Indoleamine 2,3-Dioxygenase Inhibitor Bearing an Eight-Membered Ring Fused Indole Scaffold and Its Structure-Activity Relationship

Ayuta Yamaguchi, Shinsuke Inuki,* Katsumi Ohta, Shinya Oishi, Akira Asai, and Hiroaki Ohno*

*Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan

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.