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

…, J Du Ha, SY Chu, SH Jung, YS Jung, JY Baek…

文献索引：Ahn, Jin Hee; Cho, Sung Yun; Ha, Jae Du; Chu, So Young; Jung, Sun Ho; Jung, Yoon Sung; Baek, Ji Yoen; Choi, In Kyung; Shin, Eun Young; Kang, Seung Kyu; Kim, Sung Soo; Cheon, Hyae Gyeong; Yang, Sung-Don; Choi, Joong-Kwon Bioorganic and medicinal chemistry letters, 2002 , vol. 12, # 15 p. 1941 - 1946

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被引用次数: 62

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 R4 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 ...