期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 57, 期 -, 页码 10-20出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.09.015
关键词
PTP1B; TCPTP; Diabetes; Cytotoxicity
资金
- National Comprehensive Technology Platforms for Innovative Drug RD [2009ZX09301-007]
- Special Research Fund to Doctoral Program of College and University [20110073120081]
Thirty-two 2-substituted ethenesulfonic acid ester derivatives were designed, synthesized, and evaluated for their inhibitory activities against protein tyrosine phosphatase 1B (PTP1B) and selectivity over T-Cell protein tyrosine phosphatase (TCPTP). Preliminary structure activity relationship studies demonstrated that the substitution at the aromatic center and the length of linker between the hydrophobic tail and aromatic center markedly affected the inhibitory activity against PTP1B and the selectivity over TCPTP. Specifically, compounds 43 and 36 revealed excellent inhibitory activity to PTP1B with IC50 = 1.3 mu M and 1.5 mu M, respectively, and marked 10- and 20-fold selectivity over TCPTP. Cytotoxicity data showed low cytotoxicity for COS-7 cell with IC50 values >100 mu M for most synthesized chemicals. (C) 2012 Elsevier Masson SAS. All rights reserved.
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