Synthesis and PTP1B inhibition of 1,2-naphthoquinone derivatives as potent anti-diabetic agents |
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Authors: | 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 |
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Affiliation: | Medicinal Science Division, Korea Research Institute of Chemical Technology, Taejon 305-600, Republic of Korea. |
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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. |
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