Structure-activity relationship study of 9-aminoacridine compounds in scrapie-infected neuroblastoma cells

Barnaby C.H. May, Juanita Witkop, John Sherrill, Marc O. Anderson, Peter B. Madrid, Julie A. Zorn, Stanley B. Prusiner, Fred E. Cohen, R. Kiplin Guy

Research output: Contribution to journalArticlepeer-review

28 Scopus citations

Abstract

A focused library of variously substituted 9-aminoacridine compounds was screened for bioactivity against accumulation of the infectious prion protein isoform, denoted PrPSc, in a cell model of prion replication. The efficacy of compounds against PrPSc accumulation was influenced by both substituents of the distal tertiary amine and acridine heterocycle, while cellular cytotoxicity was encoded in the acridine heterocycle substituents.

Original languageEnglish
Pages (from-to)4913-4916
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number18
DOIs
StatePublished - Sep 15 2006

Bibliographical note

Funding Information:
This work was supported by grants from the National Institutes of Health (AG02132, AG10770, and AG021601) as well as by a gift from the G. Harold and Leila Y. Mathers Charitable Foundation. S.B.P. has financial interest in InPro Biotechnology, Inc.

Keywords

  • 9-Aminoacridine
  • PrP
  • PrP
  • PrP
  • Prion
  • Quinacrine
  • ScN2a

ASJC Scopus subject areas

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

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