| Synthesis and structure-activity relationship of 5-substituent-2(1H)-pyridone derivatives as anti-fibrosis agents. | |
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MedLine Citation:
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PMID: 22342629 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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Pyridone compounds, such as pirfenidone (PFD) and fluorofenidone (AKF-PD), are multi-target anti-fibrotic agents. Using PFD and AKF-PD as the leading compounds, two series of novel (5-substituent)-2(1H)-pyridone compounds were synthesized with the purpose of maintaining multi-targeting property and overcoming the drawbacks of fast metabolism. These derivatives demonstrated good proliferation inhibiting activity against NIH3T3 cells by MTT assay with AKF-PD as the positive control. Compound 5b exhibited a high potent of anti-fibrosis with a IC(50) of 0.08mmol/L about 34 times of AKF-PD. The SAR of pyridone derivatives as anti-fibrosis agents was also discussed. |
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Authors:
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Jun Chen; Miao-Miao Lu; Bin Liu; Zhuo Chen; Qian-Bin Li; Li-Jian Tao; Gao-Yun Hu |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2012-1-28 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: - ISSN: 1464-3405 ISO Abbreviation: - Publication Date: 2012 Jan |
Date Detail:
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Created Date: 2012-2-20 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, School of Pharmacy, Central South University, Changsha, Hunan Province 410013, China. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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