Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y2 receptor antagonists

Bioorg Med Chem Lett. 2008 Jan 1;18(1):223-7. doi: 10.1016/j.bmcl.2007.10.082. Epub 2007 Oct 30.


A library of anilinoanthraquinone derivatives was synthesized by parallel Ullmann coupling reaction of bromaminic acid with aniline derivatives in solution using a compact parallel synthesizer. The products were purified by HPLC and evaluated as antagonists at mouse and human P2Y2 receptors. 4-Phenylamino-substituted 1-amino-2-sulfoanthraquinones, for example, 1-amino-4-(2-methoxyphenyl)-2-sulfoanthraquinone (PSB-716), were potent P2Y2 antagonists with IC50 values in the low micromolar range.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aniline Compounds / chemical synthesis*
  • Aniline Compounds / pharmacology*
  • Animals
  • Anthraquinones / chemical synthesis*
  • Anthraquinones / pharmacology*
  • Combinatorial Chemistry Techniques
  • Humans
  • Inhibitory Concentration 50
  • Kinetics
  • Mice
  • Purinergic P2 Receptor Antagonists*
  • Receptors, Purinergic P2Y2
  • Structure-Activity Relationship


  • Aniline Compounds
  • Anthraquinones
  • P2RY2 protein, human
  • P2ry2 protein, mouse
  • Purinergic P2 Receptor Antagonists
  • Receptors, Purinergic P2Y2