Synthesis and characterization of a potent and selective protein tyrosine phosphatase inhibitor, 2-[(4-methylthiopyridin-2-yl)methylsufinyl]benzimidazole

被引:25
作者
Hamaguchi, T
Takahashi, A
Kagamizono, T
Manaka, A
Sato, M
Osada, H
机构
[1] Taisho Pharmaceut Co Ltd, Med Res Labs, Omiya, Saitama 3308530, Japan
[2] RIKEN, Inst Phys & Chem Res, Antibiot Lab, Wako, Saitama 35101, Japan
关键词
D O I
10.1016/S0960-894X(00)00539-4
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and biological activity of a series of 2-[(4-methylthiopyridin-2-yl)methylsulfinyl]benzimidazoles are described. These compounds have potent inhibitory effects against the protein tyrosine phosphatase activity of CD45. Enzymatic analysis with several phosphatases revealed that compound 5a had high specificity for CD45 compared with serine/threonine phosphatases (PP1, PP2A), tyrosine phosphatases (LAR, PTP1B and PTP-S2) and dual phosphatase (VHR). (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2657 / 2660
页数:4
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