5-Arylidene-2,4-thiazolidinediones as inhibitors of protein tyrosine phosphatases
摘要：
4-(5-Arylidene-2,4-dioxothiazolidin-3-yl)methylbenzoic acids () 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 represents an example of utilizing phosphotyrosine-mimetics to identify effective low molecular weight nonphosphorus inhibitors of PTPs. Several thiazolidinediones exhibited PTP1B 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.Graphical abstract
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关键词：
protein tyrosine phosphatases diabetes mellitus PTP1B and LMW-PTP inhibitors molecular modelling
DOI：
10.1016/j.bmc.2007.05.027
被引量：
年份：
2007
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