4.5 Article

Synthesis and SAR study of diphenylbutylpiperidines as cell autophagy inducers

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 1, Pages 234-239

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.11.029

Keywords

Autophagy; Diphenylbutylpiperidines; Synthesis; SAR study; Inducers

Funding

  1. National Natural Science Foundation of China [21072212]
  2. National Institute of Health of US

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A novel series of diphenylbutylpiperidines as autophagy inducers was described and extensive SAR studies resulted in derivatives (15d-e, 15i-j) with 10-fold greater activity than the lead compounds 1 and 2. Meanwhile, a new synthetic route to diphenylbutyl bromide (6) from bromobenzene and gamma-butyrolactone was also reported here. (C) 2010 Elsevier Ltd. All rights reserved.

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