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Bioorg Med Chem. 2007 Aug 1;15(15):5137-49. Epub 2007 May 17.

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

Author information

1
Dipartimento Farmaco-Chimico, Università di Messina, Vl SS Annunziata, Messina, Italy. rmaccari@pharma.unime.it

Abstract

4-(5-Arylidene-2,4-dioxothiazolidin-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 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.

PMID:
17543532
DOI:
10.1016/j.bmc.2007.05.027
[Indexed for MEDLINE]

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