2. Academic Validation
  3. S-benzylisothiourea derivatives as small-molecule inhibitors of indoleamine-2,3-dioxygenase

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

  • Bioorg Med Chem Lett. 2010 Sep 1;20(17):5126-9. doi: 10.1016/j.bmcl.2010.07.025.
Kenji Matsuno 1,  Kazushige Takai,  Yoshinobu Isaka,  Yuka Unno,  Masayuki Sato,  Osamu Takikawa,  Akira Asai
Affiliations

Affiliation

  • 1 Graduate School of Pharmaceutical Sciences, University of Shizuoka, Suruga-ku, Shizuoka, Japan.
PMID: 20688518 DOI: 10.1016/j.bmcl.2010.07.025
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.

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