Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): Kinase profiling guided optimization of a 1,2,3-benzotriazole lead

Structure and kinase profiling guided the optimization of a CDK2 1,2,3-benzotriazole hit to give a series of indoles that are selective and potent dual JNK1 and 2 inhibitors. An advanced compound, 24f (IC50 JNK1/2=16/66nM), was developed and suitable for in vivo pharmacological evaluation of JNK inh...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2013-03, Vol.23 (5), p.1486-1492
Hauptverfasser:	Palmer, Wylie S., Alam, Muzaffar, Arzeno, Humberto B., Chang, Kung-Ching, Dunn, James P., Goldstein, David M., Gong, Leyi, Goyal, Bindu, Hermann, Johannes C., Hogg, J. Heather, Hsieh, Gary, Jahangir, Alam, Janson, Cheryl, Jin, Sue, Ursula Kammlott, R., Kuglstatter, Andreas, Lukacs, Christine, Michoud, Christophe, Niu, Linghao, Reuter, Deborah C., Shao, Ada, Silva, Tania, Trejo-Martin, Teresa A., Stein, Karin, Tan, Yun-Chou, Tivitmahaisoon, Parcharee, Tran, Patricia, Wagner, Paul, Weller, Paul, Wu, Shao-Yong
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals bioavailability c-Jun N-terminal kinase (JNK) CDK chemistry Crystallography, X-Ray cyclin-dependent kinase Drug Design drugs Humans JNK Mitogen-Activated Protein Kinases - antagonists & inhibitors JNK Mitogen-Activated Protein Kinases - metabolism Kinase inhibitor Kinase selectivity mitogen-activated protein kinase Models, Molecular Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Rats Structure-Activity Relationship Triazoles - chemical synthesis Triazoles - chemistry Triazoles - pharmacology
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Schreiben Sie den ersten Kommentar!