Parallel synthesis, evaluation, and preliminary structure-activity relationship of 2,5-diamino-1,4-benzoquinones as a novel class of bivalent anti-prion compound

J Med Chem. 2010 Nov 25;53(22):8197-201. doi: 10.1021/jm100882t. Epub 2010 Nov 3.

Abstract

A library of 11 entries, featuring a 2,5-diamino-1,4-benzoquinones nucleus as spacer connecting two aromatic prion recognition motifs, was designed and evaluated against prion infection. Notably, 6-chloro-1,2,3,4-tetrahydroacridine 10 showed an EC(50) of 0.17 μM, which was lower than that displayed by reference compound BiCappa. More importantly, 10 possessed the capability to contrast prion fibril formation and oxidative stress, together with a low cytotoxicity. This study further corroborates the bivalent strategy as a viable approach to the rational design of anti-prion chemical probes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acridines / chemical synthesis*
  • Acridines / chemistry
  • Acridines / pharmacology
  • Amines / chemical synthesis*
  • Amines / chemistry
  • Amines / pharmacology
  • Animals
  • Benzoquinones / chemical synthesis*
  • Benzoquinones / chemistry
  • Benzoquinones / pharmacology
  • Cell Line
  • Cell Survival / drug effects
  • Mice
  • Oxidative Stress / drug effects
  • PrPSc Proteins / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • 6-chloro-1,2,3,4-tetrahydroacridine
  • Acridines
  • Amines
  • Benzoquinones
  • PrPSc Proteins