α-Bromoacetophenone derivatives as neutral protein tyrosine phosphatase inhibitors:: Structure-activity relationship

被引：40

作者：

Arabaci, G

Yi, T

Fu, H

Porter, ME

Beebe, KD

Pei, DH

机构：

[1] Ohio State Univ, Dept Chem, Columbus, OH 43210 USA

[2] Ohio State Univ, Ohio State Biochem Program, Columbus, OH 43210 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 21期

关键词：

D O I：

10.1016/S0960-894X(02)00681-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of alpha-haloacetophenone derivatives was tested for inhibition of protein tyrosine phosphatases SHP-1 and PTP1B. The results show that the bromides are much more potent than the corresponding chlorides, whereas the phenyl ring is remarkably tolerant to modifications. Derivatization of the phenyl ring with a tripeptide Gly-Glu-Glu resulted in a potent, selective inhibitor against PTP1B. (C) 2002 Elsevier Science Ltd. All rights reserved.

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页码：3047 / 3050

页数：4

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