Format

Send to

Choose Destination
Bioorg Med Chem. 2006 Apr 1;14(7):2162-77. Epub 2005 Nov 21.

Bicyclic and tricyclic thiophenes as protein tyrosine phosphatase 1B inhibitors.

Author information

1
Chemical and Screening Science, Wyeth Research, 200 Cambridge Park Drive, Cambridge, MA 02140, USA.

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.

PMID:
16303309
DOI:
10.1016/j.bmc.2005.11.005
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center