Title of article
Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells
Author/Authors
Mark C. Bagley، نويسنده , , Terence Davis، نويسنده , , Matthew C. Dix، نويسنده , , Michal J. Rokicki، نويسنده , , David Kipling، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
5107
To page
5110
Abstract
The p38 mitogen-activated protein kinase inhibitor VX-745 is prepared rapidly and efficiently in a four-step sequence using a combination of conductive heating and microwave-mediated steps. Its inhibitory activity was confirmed in hTERT immortalized HCA2 and WS dermal fibroblasts at 0.5–1.0 μM concentration by ELISA and immunoblot assay, and displays excellent kinase selectivity over the related stress-activated kinase JNK.
Keywords
Heterocycles , p38 MAPK , Palladium , Werner syndrome , VX-745 , microwaves , Ullmann coupling
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798562
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