Bioorganic & Medicinal Chemistry Letters 2002-08-05

Synthesis and PTP1B inhibition of 1,2-naphthoquinone derivatives as potent anti-diabetic agents.

Jin Hee Ahn, Sung Yun Cho, Jae Du Ha, So Young Chu, Sun Ho Jung, Yoon Sung Jung, Ji Yoen Baek, In Kyung Choi, Eun Young Shin, Seung Kyu Kang, Sung Soo Kim, Hyae Gyeong Cheon, Sung-Don Yang, Joong-Kwon Choi

文献索引：Bioorg. Med. Chem. Lett. 12(15) , 1941-6, (2002)

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摘要

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.