Selective opioid growth factor receptor antagonists based on a stilbene isostere

David P. Stockdale, Michelle B. Titunick, Jessica M. Biegler, Jessie L. Reed, Alyssa M. Hartung, David F. Wiemer, Patricia J. McLaughlin, Jeffrey D. Neighbors

Research output: Contribution to journalArticlepeer-review

6 Scopus citations


As part of an ongoing drug development effort aimed at selective opioid receptor ligands based on the pawhuskin natural products we have synthesized a small set of amide isosteres. These amides were centered on lead compounds which are selective antagonists for the delta and kappa opioid receptors. The amide isomers revealed here show dramatically different activity from the parent stilbene compounds. Three of the isomers synthesized showed antagonist activity for the opioid growth factor (OGF)/opioid growth factor receptor (OGFR) axis which is involved in cellular and organ growth control. This cellular signaling mechanism is targeted by “low-dose” naltrexone therapy which is being tested clinically for multiple sclerosis, Crohn's disease, cancer, and wound healing disorders. The compounds described here are the first selective small molecule ligands for the OGF/OGFR system and will serve as important leads and probes for further study.

Original languageEnglish (US)
Pages (from-to)4464-4474
Number of pages11
JournalBioorganic and Medicinal Chemistry
Issue number16
StatePublished - 2017

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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