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Design, synthesis, and evaluation of bromo-retrochalcone derivatives as protein tyrosine phosphatase 1B inhibitors |
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| Authors: | Liu Zhiguo Lee Woojung Kim Su-Nam Yoon Goo Cheon Seung Hoon |
| Institution: | a College of Pharmacy and Research Institute of Drug Development, Chonnam National University, 300 Yongbong-Dong, Buk-Gu, Gwangju 500-757, Republic of Korea b KIST Gangneung Institute, Gangneung 210-340, Republic of Korea c College of Pharmacy, Mokpo National University, 1666 Youngsan-ro, Cheonggye-myeon, Muan-gun, Jeonnam, Republic of Korea |
| Abstract: | A series of bromo-retrochalcones was designed, synthesized and evaluated as PTP1B inhibitors based on licochalcone A and E. Compounds 6, 12, 13, 14, 25, 36, 37, 39, and 41 showed potent inhibitory effects against PTP1B, and compound 37, the most potent among the series, had an IC50 value of 1.9 μM, about two-fold better than that of the positive control, ursolic acid. |
| Keywords: | Bromo-retrochalcone Protein tyrosine phosphatase 1B Licochalcone Synthetic |
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