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

被引：40

作者：

Matsuno, Kenji ^{[1
]}

Takai, Kazushige ^{[1
]}

Isaka, Yoshinobu ^{[1
]}

Unno, Yuka ^{[1
]}

Sato, Masayuki ^{[1
]}

Takikawa, Osamu ^{[2
]}

Asai, Akira ^{[1
]}

机构：

[1] Univ Shizuoka, Grad Sch Pharmaceut Sci, Suruga Ku, Shizuoka 4228526, Japan

[2] Natl Ctr Geriatr & Gerontol, Natl Inst Longev Sci, Aichi 4748522, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 17期

关键词：

SAR; IDO; Tryptophan; Kynurenine; Cancer; HUMAN INDOLEAMINE 2,3-DIOXYGENASE; COMPETITIVE INHIBITORS; TRYPTOPHAN-METABOLISM; BINDING; CELLS; DIOXYGENASE; EXPRESSION; TOLERANCE; MECHANISM; CANCER;

D O I：

10.1016/j.bmcl.2010.07.025

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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-mu M 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. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：5126 / 5129

页数：4

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