104408-29-9Relevant articles and documents
Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): Kinase profiling guided optimization of a 1,2,3-benzotriazole lead
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,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
, p. 1486 - 1492 (2013)
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 J
Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): Optimization for JNK potency and physicochemical properties
Gong, Leyi,Han, Xiaochun,Silva, Tania,Tan, Yun-Chou,Goyal, Bindu,Tivitmahaisoon, Parch,Trejo, Alejandra,Palmer, Wylie,Hogg, Heather,Jahagir, Alam,Alam, Muzaffar,Wagner, Paul,Stein, Karin,Filonova, Lubov,Loe, Brad,Makra, Ferenc,Rotstein, David,Rapatova, Lubica,Dunn, James,Zuo, Fengrong,Porto, Joseph Dal,Wong, Brian,Jin, Sue,Chang, Alice,Tran, Patricia,Hsieh, Gary,Niu, Linghao,Shao, Ada,Reuter, Deborah,Hermann, Johaness,Kuglstatter, Andreas,Goldstein, David
, p. 3565 - 3569 (2013/07/28)
A novel series of indole/indazole-aminopyrimidines was designed and synthesized with an aim to achieve optimal potency and selectivity for the c-Jun kinase family or JNKs. Structure guided design was used to optimize the series resulting in a significant potency improvement. The best compound (17) has IC50 of 3 nM for JNK1 and 20 nM for JNK2, with greater than 40-fold selectivity against other kinases with good physicochemical and pharmacokinetic properties.
Inhibitors of JNK
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Page/Page column 40, (2011/02/26)
The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein p, q, Y′, r, Rsup