| Multisubstituted quinoxalines and pyrido[2,3-d]pyrimidines: Synthesis and SAR study as tyrosine kinase c-Met inhibitors. | |
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MedLine Citation:
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PMID: 22985853 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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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. |
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Authors:
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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:
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Type: JOURNAL ARTICLE Date: 2012-8-27 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: - ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2012 Aug |
Date Detail:
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Created Date: 2012-9-18 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2012 Elsevier Ltd. All rights reserved. |
Affiliation:
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Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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