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ID: ALA1135185
Journal: Bioorg Med Chem Lett
Title: Synthesis and PTP1B inhibition of 1,2-naphthoquinone derivatives as potent anti-diabetic agents.
Authors: Ahn JH, Cho SY, Ha JD, Chu SY, Jung SH, Jung YS, Baek JY, Choi IK, Shin EY, Kang SK, Kim SS, Cheon HG, Yang SD, Choi JK.
Abstract: A new series of 1,2-naphthoquinone derivatives was synthesized by various synthetic methods and evaluated for their ability to inhibit protein tyrosine phosphatase 1B (PTP1B). 1,2-Naphthoquinone derivatives with substituent at R(4) position showed submicromolar inhibitory activity, and compound 24 demonstrated 10- to 60-fold selectivity against the tested phosphatases. Also, several 4-aryl-1,2-naphthoquinone derivatives with substituents at R(3), R(6), R(7), or/and R(8) showed submicromolar inhibitory activity and good plasma stability.
CiteXplore: 12113814