Discovery and Synthesis of a Novel Series of Liver X Receptor Antagonists

• Nian Siyun

  Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry

• Gan Xia

  Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry

• Tan Xiangduan

  College of Pharmacy, Guilin Medical University

• Yu Zhenpeng

  Shanghai Shyndec Pharmaceutical Co., Ltd.

• Wang Panfeng

  Shanghai Shyndec Pharmaceutical Co., Ltd.

• Chen Xing

  Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry

• Wang Guoping

  Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry Shanghai Shyndec Pharmaceutical Co., Ltd.

抄録

Fourteen novel compounds were prepared and their antagonistic activities against liver X receptors (LXR) α/β were tested in vitro. Compound 26 had an IC₅₀ value of 6.4 µM against LXRα and an IC₅₀ value of 5.6 µM against LXRβ. Docking studies and the results of structure–activity relationships support the further development of this chemical series as LXRα/β antagonists.

収録刊行物

• ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ

  ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 63 (8), 628-635, 2015

  公益社団法人 日本薬学会

キーワード

• liver X receptor α
• liver X receptor β
• antagonistic activity

詳細情報

• CRID: 1390282679153693440
• NII論文ID: 130005090105
• NII書誌ID: AA00602100
• DOI: 10.1248/cpb.c15-00261
• ISSN: 13475223
• ISSN: 00092363
• NDL書誌ID: 026616884
• PubMed: 26062802
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I026616884
• Web Site: https://www.jstage.jst.go.jp/article/cpb/63/8/63_c15-00261/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2016128333
• 本文言語コード: en
• データソース種別:
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  • NDL
  • Crossref
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  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可