Document Detail

Multisubstituted quinoxalines and pyrido[2,3-d]pyrimidines: Synthesis and SAR study as tyrosine kinase c-Met inhibitors.
MedLine Citation:
PMID:  22985853     Owner:  NLM     Status:  Publisher    
Two series of new analogues were designed by replacing the quinoline scaffold of our earlier lead 2 (zgwatinib) with quinoxaline and pyrido[2,3-d]pyrimidine frameworks. Moderate c-Met inhibitory activity was observed in the quinoxaline series. Among the pyrido[2,3-d]pyrimidine series, compounds 13a-c possessing an O-linkage were inactive, whilst the N-linked analogues 15a-c retained c-Met inhibitory potency. Highest activity was observed in the 3-nitrobenzyl analog 15b that showed an IC(50) value of 6.5nM. Further structural modifications based on this compound were undergoing.
Kui Wu; Jing Ai; Qiufeng Liu; Tiantian Chen; Ailing Zhao; Xia Peng; Yuanxiang Wang; Yinchun Ji; Qizheng Yao; Yechun Xu; Meiyu Geng; Ao Zhang
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-8-27
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  -     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2012 Aug 
Date Detail:
Created Date:  2012-9-18     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2012 Elsevier Ltd. All rights reserved.
Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
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