5-arylidene-2,4-thiazolidinediones as inhibitors of protein tyrosine phosphatases

被引：106

作者：

Maccari, Rosanna ^{[1
]}

Paoli, Paolo

Ottana, Rosaria

Jacomelli, Michela

Ciurleo, Rosella

Manao, Giampaolo

Steindl, Theodora

Langer, Thierry

Vigorita, Maria Gabriella

Camici, Guido

机构：

[1] Univ Messina, Dipartimento Farmacochim, I-98168 Messina, Italy

[2] Univ Florence, Dipartimento Sci Biochim, I-50134 Florence, Italy

[3] Univ Innsbruck, Dept Pharmaceut Chem, Inst Pharm, A-6020 Innsbruck, Austria

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2007年 / 15卷 / 15期

关键词：

protein tyrosine phosphatases; diabetes mellitus; PTP1B and LMW-PTP inhibitors; molecular modelling;

D O I：

10.1016/j.bmc.2007.05.027

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

4-(5-Arylidene-2,4-dioxothiszolidin-3-yl)methylbenzoic acids (2) were synthesized and evaluated in vitro as inhibitors of PTP1B and LMW-PTP, two protein tyrosine phosphatases (PTPs) which act as negative regulators of the metabolic and mitotic signalling of insulin. The synthesis of compounds 2 represents an example of utilizing phosphotyrosine-mimetics to identify effective low molecular weight nonphosphorus inhibitors of PTPs. several thiazolidinediones 2 exhibited PTP1 B inhibitory activity in the low micromolar range with moderate selectivity for human PTP1B and IF1 isoform of human LMW-PTP compared with other related PTPs. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：5137 / 5149

页数：13

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