作者
Rosanna Maccari, Paolo Paoli, Rosaria Ottanà, Michela Jacomelli, Rosella Ciurleo, Giampaolo Manao, Theodora Steindl, Thierry Langer, Maria Gabriella Vigorita, Guido Camici
发表日期
2007/8/1
期刊
Bioorganic & medicinal chemistry
卷号
15
期号
15
页码范围
5137-5149
出版商
Pergamon
简介
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.
引用总数
20082009201020112012201320142015201620172018201920202021202220232024413651415111358111135634
学术搜索中的文章
R Maccari, P Paoli, R Ottanà, M Jacomelli, R Ciurleo… - Bioorganic & medicinal chemistry, 2007