| Novel nonsecosteroidal vitamin D(3) carboxylic acid analogs for osteoporosis, and SAR analysis. | |
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MedLine Citation:
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PMID: 21795053 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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Novel vitamin D(3) analogs with carboxylic acid were explored, focusing on a nonsecosteroidal analog, LG190178, with a bisphenyl skeleton. From X-ray analysis of these analogs with vitamin D receptor (VDR), the carboxyl groups had very unique hydrogen bonding interactions in VDR and mimicked 1α-hydroxy group and/or 3β-hydroxy group of 1α,25-dihydroxyvitamin D(3). A highly potent analog, 6a, with good in vitro activity and pharmacokinetic profiles was identified from an SAR study. Compound 6a showed significant prevention of bone loss in a rat osteoporosis model by oral administration. |
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Authors:
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Hirotaka Kashiwagi; Yoshiyuki Ono; Kazuki Shimizu; Tsuyoshi Haneishi; Susumu Ito; Shigeyuki Iijima; Takamitsu Kobayashi; Fumihiko Ichikawa; Suguru Harada; Hideki Sato; Nobuo Sekiguchi; Masaki Ishigai; Tadakatsu Takahashi |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-7-8 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry Volume: - ISSN: 1464-3391 ISO Abbreviation: - Publication Date: 2011 Jul |
Date Detail:
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Created Date: 2011-7-28 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9413298 Medline TA: Bioorg Med Chem Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2011 Elsevier Ltd. All rights reserved. |
Affiliation:
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Research Division, Chugai Pharmaceutical Co. Ltd, 1-135 Komakado, Gotemba, Shizuoka 412-8513, Japan. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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