期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 29, 期 10, 页码 1187-1193出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.03.023
关键词
PTP1B inhibitor; 1,3-Diphenyl-1H-pyrazole; Rhodanine-3-alkanoic acid
资金
- National Natural Science Foundation of China [81460524, 81773779]
- Education Department of Jilin Province Scientific Research Fund Project, China [2015-50]
- Edanz Group China
Two series of 1,3-diphenyl-1H-pyrazole derivatives containing rhodanine-3-alkanoic acid groups were identified as competitive protein tyrosine phosphatase 1B (PTP1B) inhibitors. Among the compounds studied, IIIv was found to have the best in vitro inhibition activity against PTP1B (IC50 = 0.67 +/- 0.09 mu M) and the best selectivity (9-fold) between PTP1B and T-cell protein tyrosine phosphatase (TCPTP). Molecular docking studies demonstrated that compounds IIIm, IIIv and IVg could occupy simultaneously at both the catalytic site and the adjacent pTyr binding site. These results provide novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
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