Anthraquinones as a privileged scaffold in drug discovery targeting nucleotide-binding proteins

Abstract

Anthraquinones are condensed aromatic hydrocarbons found naturally in medicinal plants and known for their potential medical and dye applications. Anthraquinones were developed as P2 receptor antagonists and ectonucleotidase inhibitors and feature very different characteristic properties regarding the binding site for anthraquinones. This demonstrates that the anthraquinone scaffold appears to behave as a privileged structure in medicinal chemistry targeting nucleotide-binding proteins, and the substitution pattern, especially in the 4-position, can direct its interaction with specific targets. This article will cover the structure activity relationships of anthraquinones for three different targets: P2Y12 receptor, ecto-5'-nucleotidase and P2X2 receptor.