| Synthesis, anti-HBV activity and renal cell toxicity evaluation of mixed phosphonate prodrugs of adefovir. | |
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MedLine Citation:
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PMID: 22305613 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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A series of phosphonate ester prodrugs of adefovir incorporating l-amino (thio)acid and non-steroidal anti-inflammatory drug (NSAID) moieties were synthesized and their anti-HBV activity and renal cell toxicity were evaluated in HepG2 2.2.15 and HK-2 cells respectively. Bioactivity evaluation results revealed that this kind of adefovir prodrug have lower renal cell toxicity than adefovir dipivoxil. Compounds 8a and 8b, incorporating the NSAID ketoprofen and the l-amino acid (Val or Ile) structural fragments, exhibited more potent anti-HBV activity than adefovir dipivoxil with IC(50) = 0.51 and 0.73 μM, SI = 1697.64 and 881.92 respectively. In vitro stability studies showed that the synthesized prodrugs have higher chemical and plasma stability than the positive control adefovir dipivoxil. |
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Authors:
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Xiao-Zhong Fu; Yu Ou; Jian-Ying Pei; Ying Liu; Jing Li; Wen Zhou; Yan-Yu Lan; Ai-Min Wang; Yong-Lin Wang |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2012-1-14 |
Journal Detail:
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Title: European journal of medicinal chemistry Volume: - ISSN: 1768-3254 ISO Abbreviation: - Publication Date: 2012 Jan |
Date Detail:
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Created Date: 2012-2-6 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0420510 Medline TA: Eur J Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2012 Elsevier Masson SAS. All rights reserved. |
Affiliation:
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School of Pharmacy, Guiyang Medical College, 9 Beijing Road, Guiyang, Guizhou 550004, PR China. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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