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.

5-Arylidene- 2,4-Thiazolidinediones Inhibitors of Protein Tyrosine Phosphatases / R.Maccari; P.Paoli; R.Ottanà; M.Jacomelli; R.Ciurleo; G.Manao; T.Steindl; T.Langer; M.Vigorita; G.Camici. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 1464-3391. - STAMPA. - 15:(2007), pp. 5137-5149. [10.1016/j.bmc.2007.05.027]

5-Arylidene- 2,4-Thiazolidinediones Inhibitors of Protein Tyrosine Phosphatases

PAOLI, PAOLO;MANAO, GIAMPAOLO;CAMICI, GUIDO
2007

Abstract

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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5137
5149
R.Maccari; P.Paoli; R.Ottanà; M.Jacomelli; R.Ciurleo; G.Manao; T.Steindl; T.Langer; M.Vigorita; G.Camici
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2158/315501
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