Synthesis and characterization of a potent and selective protein tyrosine phosphatase inhibitor, 2.
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).
Hamaguchi
T
T
Medical Research Laboratories, Taisho Pharmaceutical Co., Ltd, Saitama, Japan. s14795@ccm.taisho.co.jp
Takahashi
A
A
Kagamizono
T
T
Manaka
A
A
Sato
M
M
Osada
H
H
D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017493:Leukocyte Common Antigens / Q000378:metabolism; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013454:Sulfoxides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
C419888:2-((4-methylthiopyridin-2-yl)methylsulfinyl)benzimidazole; D001562:Benzimidazoles; D004791:Enzyme Inhibitors; D013454:Sulfoxides; D017493:Leukocyte Common Antigens; D017027:Protein Tyrosine Phosphatases