2. Academic Validation
  3. Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y2 receptor antagonists

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.
Stefanie Weyler 1,  Younis Baqi,  Petra Hillmann,  Marko Kaulich,  Andrea M Hunder,  Ingrid A Müller,  Christa E Müller
Affiliations

Affiliation

  • 1 Pharmaceutical Institute, Pharmaceutical Sciences Bonn, University of Bonn, An der Immenburg 4, D-53121 Bonn, Germany.
PMID: 18006312 DOI: 10.1016/j.bmcl.2007.10.082
Abstract

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.

Figures