Formylchromone derivatives as a novel class of protein tyrosine phosphatase 1B inhibitors

YS Shim, KC Kim, DY Chi, KH Lee, H Cho

文献索引：Shim, Yi Sup; Kim, Ki Chul; Chi, Dae Yoon; Lee, Keun-Hyeung; Cho, Hyeongjin Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 15 p. 2561 - 2563

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被引用次数: 76

摘要

Formylchromone inhibits a human protein tyrosine phosphatase PTP1B with a IC50 value of 73 μM. The chemical reactivity of formylchromone was adjusted by substitution at various positions of the formylchromone skeleton. In an initial assessment of the structure–activity relationship, the most potent inhibitor showed an IC50 of 4.3 μM against PTP1B and strong or medium selectivity against other human PTPases, LAR and TC-PTP. This compound, ...