Autor: |
R. Ursula Kammlott, Deborah Carol Reuter, Teresa Alejandra Trejo-Martin, Leyi Gong, Christophe Michoud, Andreas Kuglstatter, Patricia Tran, David Michael Goldstein, Yun-Chou Tan, Parcharee Tivitmahaisoon, Linghao Niu, Shao-Yong Wu, Sue Jin, Paul Weller, Gary Hsieh, Karin Ann Stein, Humberto Bartolome Arzeno, James Patrick Dunn, Ada Shao, Wylie Solang Palmer, J. Heather Hogg, Johannes C. Hermann, Kung-ching Chang, Bindu Goyal, Alam Jahangir, Cheryl Janson, Tania Silva, Christine Lukacs, Paul J. Wagner, Muzaffar Alam |
Rok vydání: |
2013 |
Předmět: |
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Zdroj: |
Bioorganic & Medicinal Chemistry Letters. 23:1486-1492 |
ISSN: |
0960-894X |
Popis: |
A series of amino-pyrimidines was developed based upon an initial kinase cross-screening hit from a CDK2 program. Kinase profiling and structure-based drug design guided the optimization from the initial 1,2,3-benzotriazole hit to a potent and selective JNK inhibitor, compound 24f (JNK1 and 2 IC(50)=16 and 66 nM, respectively), with bioavailability in rats and suitable for further in vivo pharmacological evaluation. |
Databáze: |
OpenAIRE |
Externí odkaz: |
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