Author/Authors :
Jin-Hee Ahn، نويسنده , , Sung Yun Cho، نويسنده , , Jae Du Ha، نويسنده , , So Young Chu، نويسنده , , Sun Ho Jung، نويسنده , , Yoon Sung Jung، نويسنده , , Ji Yoen Baek، نويسنده , , In Kyung Choi، نويسنده , , Eun Young Shin، نويسنده , , Seung Kyu Kang، نويسنده , , Sung-Soo Kim، نويسنده , , Hyae Gyeong Cheon، نويسنده , , Sung-Don Yang، نويسنده , , Joong-Kwon Choi، نويسنده ,
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 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 R3, R6, R7, or/and R8 showed submicromolar inhibitory activity and good plasma stability.
