| Literature DB >> 21316234 |
Simeon Bowers1, Anh P Truong, R Jeffrey Neitz, Martin Neitzel, Gary D Probst, Roy K Hom, Brian Peterson, Robert A Galemmo, Andrei W Konradi, Hing L Sham, Gergley Tóth, Hu Pan, Nanhua Yao, Dean R Artis, Elizabeth F Brigham, Kevin P Quinn, John-Michael Sauer, Kyle Powell, Lany Ruslim, Zhao Ren, Frédérique Bard, Ted A Yednock, Irene Griswold-Prenner.
Abstract
The SAR of a series of tri-substituted thiophene JNK3 inhibitors is described. By optimizing both the N-aryl acetamide region of the inhibitor and the 4-position of the thiophene we obtained single digit nanomolar compounds, such as 47, which demonstrated an in vivo effect on JNK activity when dosed orally in our kainic acid mouse model as measured by phospho-c-jun reduction.Entities:
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Year: 2011 PMID： 21316234 DOI： 10.1016/j.bmcl.2011.01.046
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823