- Synthesis and PTP1B inhibition of 1,2-naphthoquinone derivatives as potent anti-diabetic agents.
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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.
- 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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p. 1941 - 1946
(2007/10/03)
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