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Novel Notch-sparing gamma-secretase inhibitors derived from a peroxisome proliferator-activated receptor agonist library

  作者 Kurosumi, M; Nishio, Y; Osawa, S; Kobayashi, H; Iwatsubo, T; Tomita, T; Miyachi, H  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2010年20-17;  页码  5282-5285  
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[摘要]Screening of our library of peroxisome proliferator-activated receptor (PPAR) agonists yielded several phenylpropanoic acid-derived gamma-secretase inhibitors (GSIs). Structure-activity relationship studies indicated that (R)-configuration of alpha-substituted phenylpropanoic acid structure and cinnamic acid structure is favorable to prepare Notch-sparing GSIs. (C) 2010 Elsevier Ltd. All rights reserved.

 
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