1263479-95-3Relevant articles and documents
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.