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

被引：67

作者：

Ahn, JH ^{[1
]}

Cho, SY ^{[1
]}

Ha, JD ^{[1
]}

Chu, SY ^{[1
]}

Jung, SH ^{[1
]}

Jung, YS ^{[1
]}

Baek, JY ^{[1
]}

Choi, IK ^{[1
]}

Shin, EY ^{[1
]}

Kang, SK ^{[1
]}

Kim, SS ^{[1
]}

Cheon, HG ^{[1
]}

Yang, SD ^{[1
]}

Choi, JK ^{[1
]}

机构：

[1] Korea Res Inst Chem Technol, Div Med Sci, Taejon 305600, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(02)00331-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

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. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：1941 / 1946

页数：6

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