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

Kenji Matsuno, Kazushige Takai, Yoshinobu Isaka, Yuka Unno, Masayuki Sato, Osamu Takikawa, Akira Asai

Research output: Contribution to journalArticlepeer-review

40 Citations (Scopus)


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-μM 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.

Original languageEnglish
Pages (from-to)5126-5129
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number17
Publication statusPublished - 2010 Sept 1
Externally publishedYes


  • Cancer
  • IDO
  • Kynurenine
  • SAR
  • Tryptophan

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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