title: S-benzylisothiourea derivatives as small-molecule inhibitors of indoleamine-2,3-dioxygenase.
abstract: 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-muM 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.
authors.affiliation: Graduate School of Pharmaceutical Sciences, University of Shizuoka, Suruga-ku, Shizuoka, Japan.
authors.forename: Kenji
authors.initials: K
authors.lastname: Matsuno
authors.forename: Kazushige
authors.initials: K
authors.lastname: Takai
authors.forename: Yoshinobu
authors.initials: Y
authors.lastname: Isaka
authors.forename: Yuka
authors.initials: Y
authors.lastname: Unno
authors.forename: Masayuki
authors.initials: M
authors.lastname: Sato
authors.forename: Osamu
authors.initials: O
authors.lastname: Takikawa
authors.forename: Akira
authors.initials: A
authors.lastname: Asai
mesh_terms: D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D050503:Indoleamine-Pyrrole 2,3,-Dioxygenase / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D050503:Indoleamine-Pyrrole 2,3,-Dioxygenase; D013890:Thiourea