5-Arylidene-2,4-thiazolidinediones as inhibitors of protein tyrosine phosphatases |
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Authors: | Maccari Rosanna Paoli Paolo Ottanà Rosaria Jacomelli Michela Ciurleo Rosella Manao Giampaolo Steindl Theodora Langer Thierry Vigorita Maria Gabriella Camici Guido |
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Institution: | Dipartimento Farmaco-Chimico, Università di Messina, Vl SS Annunziata, Messina, Italy. rmaccari@pharma.unime.it |
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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. |
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