Title of article
Bicyclic and tricyclic thiophenes as protein tyrosine phosphatase 1B inhibitors Original Research Article
Author/Authors
A.F. Moretto، نويسنده , , S.J. Kirincich، نويسنده , , W.X. Xu، نويسنده , , M.J. Smith، نويسنده , , Z.-K. Wan، نويسنده , , D.P. Wilson، نويسنده , , B.C. Follows، نويسنده , , E. Binnun، نويسنده , , D. Joseph-McCarthy، نويسنده , , K. Foreman، نويسنده , , D.V. Erbe، نويسنده , , Y.L. Zhang، نويسنده , , S.K. Tam، نويسنده , , S.Y. Tam، نويسنده , , J. Lee، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
16
From page
2162
To page
2177
Abstract
A novel pyridothiophene inhibitor of PTP1B was discovered by rational screening of phosphotyrosine mimics at high micromolar concentrations. The potency of this lead compound has been improved significantly by medicinal chemistry guided by X-ray crystallography and molecular modeling. Excellent consistency has been observed between structure–activity relationships and structural information from PTP1B-inhibitor complexes.
Keywords
BALL-1 cells , apoptosis , Structure–activity relationships , epolactaene
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2006
Journal title
Bioorganic and Medicinal Chemistry
Record number
1305591
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