Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375789 | Bioorganic & Medicinal Chemistry Letters | 2008 | 6 Pages |
Abstract
We have synthesized and evaluated a series of triaryl sulfonamide-based PTP1B inhibitors in which a difluoro-methylenephosphonate group of a potent lead has been replaced by potential bioisosteric replacements. Several mono- or di-charged compounds (8a, 8b, and 15a) were shown exhibit inhibitory activity in the low micromolar range, demonstrating the feasibility of using this approach in identifying non-phosphonate pTyr mimetics in a small molecular scaffold. These results also provide a useful indication of the relative effectiveness of these pTyr mimetics.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Christopher P. Holmes, Xianfeng Li, Yijun Pan, Caiding Xu, Ashok Bhandari, Claire M. Moody, Joy A. Miguel, Steven W. Ferla, M. Nuria De Francisco, Brian T. Frederick, Siqun Zhou, Natalie Macher, Larry Jang, Jennifer D. Irvine, J. Russell Grove,