| Literature DB >> 23664880 |
Leyi Gong1, Xiaochun Han, Tania Silva, Yun-Chou Tan, Bindu Goyal, Parch Tivitmahaisoon, Alejandra Trejo, Wylie Palmer, Heather Hogg, Alam Jahagir, Muzaffar Alam, Paul Wagner, Karin Stein, Lubov Filonova, Brad Loe, Ferenc Makra, David Rotstein, Lubica Rapatova, James Dunn, Fengrong Zuo, Joseph Dal Porto, Brian Wong, Sue Jin, Alice Chang, Patricia Tran, Gary Hsieh, Linghao Niu, Ada Shao, Deborah Reuter, Johaness Hermann, Andreas Kuglstatter, David Goldstein.
Abstract
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.Entities:
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Year: 2013 PMID： 23664880 DOI： 10.1016/j.bmcl.2013.04.029
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823