| Literature DB >> 23142618 |
Leyi Gong1, Yun-Chou Tan, Genevieve Boice, Sarah Abbot, Kristen McCaleb, Pravin Iyer, Fengrong Zuo, Joseph Dal Porto, Brian Wong, Sue Jin, Alice Chang, Patricia Tran, Gary Hsieh, Linghao Niu, Ada Shao, Deborah Reuter, Christine M Lukacs, R Ursula Kammlott, Andreas Kuglstatter, David Goldstein.
Abstract
A novel series of highly selective JNK inhibitors based on the 4-quinolone scaffold was designed and synthesized. Structure based drug design was utilized to guide the compound design as well as improvements in the physicochemical properties of the series. Compound (13c) has an IC(50) of 62/170 nM for JNK1/2, excellent kinase selectivity and impressive efficacy in a rodent asthma model. Published by Elsevier Ltd.Entities:
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Year: 2012 PMID： 23142618 DOI： 10.1016/j.bmcl.2012.10.066
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823