Cyclic analogue of S-benzylisothiourea that suppresses kynurenine production without inhibiting indoleamine 2,3-dioxygenase activity.

Miwa Fukuda, Tomomi Sasaki,Tomoko Hashimoto,Hiroyuki Miyachi,Minoru Waki,Akira Asai,Osamu Takikawa,Osamu Ohno,Kenji Matsuno

Bioorganic & Medicinal Chemistry Letters（2018）

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摘要

•Modifying S-benzylisothiourea provided IDO inhibitors.•Cpd 2i demonstrated potent inhibition for kynurenine production.•Cpd 2i had barely effect on the enzymatic activity of IDO unexpectedly.•Cpd 2i suppressed the expression of IDO by inhibiting STAT1 expression in cells.

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关键词

Kynurenine,Inhibitor,Indoleamine 2,3-Dioxygenase,Signal transducer and activator of transcription 1,Immunological cancer treatment

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