881185-98-4Relevant articles and documents
Formylchromone derivatives as a novel class of protein tyrosine phosphatase 1B inhibitors
Shim, Yi Sup,Kim, Ki Chul,Chi, Dae Yoon,Lee, Keun-Hyeung,Cho, Hyeongjin
, p. 2561 - 2563 (2003)
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, however, was not selective against microbial PTPases, YPTP1 and YOP. The potency and selectivity of the formylchromone derivatives expecting further improvements provides a novel pharmacophore for the design of drugs for the treatmenrt of type 2 diabetes and obesity.