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S-Benzylisothiourea derivatives as small-molecule inhibitors of indoleamine-2,3-dioxygenase

✍ Scribed by Kenji Matsuno; Kazushige Takai; Yoshinobu Isaka; Yuka Unno; Masayuki Sato; Osamu Takikawa; Akira Asai

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 416 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.07.025

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✦ Synopsis

S-Benzylisothiourea 3a was discovered by its ability to inhibit indoleamine-2,3-dioxygenase (IDO) in our screening program. Subsequent optimization of the initial hit 3a lead to the identification of sub-lM inhibitors 3r and 10h, both of which suppressed kynurenine production in A431 cells. Synthesis and structure-activity relationship of S-benzylisothiourea analogues as small-molecule inhibitors of IDO are described.

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