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Short Paper | Special issue | Vol 103, No. 1, 2021, pp.511-525
Published online, 9th November, 2020
DOI: 10.3987/COM-20-S(K)35
Design, Synthesis, Physical Properties and Indoleamine 2, 3-Dioxygenase 1 Inhibitory Activity of Substituted Indole Derivatives with N-H, N-Methoxymethyl, or N-Mehylthiomethyl Group toward Fragment-Based Drug Discovery

Kenta Hayami, Yuichi Kuboki, Katsumi Ohta, Bangzhong Lin, Megumi Fumimoto, Kazuto Nunomura, Jun-Ichi Haruta , Kenichi Murai, Hiromichi Fujioka, Akira Asai, and Mitsuhiro Arisawa*

*Graduate School of Pharmaceutical Science, Osaka University, 1-6 Yamadaoka, Suita, Osaka 560-0871, Japan


We designed and prepared N-H, N-CH2OMe(MOM), and N-CH2SMe (MTM) forms of various substituted indoles, using a docking study, as a small fragment library toward fragment-based drug discovery (FBDD) and evaluated their indoleamine 2, 3-dioxygenase 1 (IDO1) inhibitory activities and physical properties.