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ID: ALA1221317

Journal: Bioorg Med Chem Lett

Title: S-benzylisothiourea derivatives as small-molecule inhibitors of indoleamine-2,3-dioxygenase.

Authors: Matsuno K, Takai K, Isaka Y, Unno Y, Sato M, Takikawa O, Asai A.

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.

CiteXplore: 20688518

DOI: 10.1016/j.bmcl.2010.07.025