2. Academic Validation
  3. Novel Notch-sparing gamma-secretase inhibitors derived from a peroxisome proliferator-activated receptor agonist library

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

  • Bioorg Med Chem Lett. 2010 Sep 1;20(17):5282-5. doi: 10.1016/j.bmcl.2010.06.131.
Motonori Kurosumi 1,  Yoshino Nishio,  Satoko Osawa,  Hisayoshi Kobayashi,  Takeshi Iwatsubo,  Taisuke Tomita,  Hiroyuki Miyachi
Affiliations

Affiliation

  • 1 Division of Pharmaceutical Sciences, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Kita-ku, Okayama, Japan.
PMID: 20650635 DOI: 10.1016/j.bmcl.2010.06.131
Abstract

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.

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