- S-benzylisothiourea derivatives as small-molecule inhibitors of indoleamine-2,3-dioxygenase.
S-benzylisothiourea derivatives as small-molecule inhibitors of indoleamine-2,3-dioxygenase.
Bioorganic & medicinal chemistry letters (2010-08-07)
Kenji Matsuno, Kazushige Takai, Yoshinobu Isaka, Yuka Unno, Masayuki Sato, Osamu Takikawa, Akira Asai
PMID20688518
摘要
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.