RSC Medicinal Chemistry Blog

This review from Stuart J. Conway and colleagues at University of Oxford and University of St Andrews, presents the major functional groups that have been employed as phosphate bioisoteres and the context of their use and deployment explained, including:

• Phosphorus-based phosphate bioisosteres
• Sulfur-based bioisosteres
• Carboxylate-based bioisosteres
• Heterocyclic-based bioisosteres
• Squaric acid and squaramide-based phosphate bioisosteres
• Phosphate bioisosteres containing other heteroatoms

Conway et al. hope that this review will provide a useful reference to medicinal chemists and chemical biologists alike who are involved in designing molecules that target phosphate-binding proteins.

The use of phosphate bioisosteres in medicinal chemistry and chemical biology
Thomas S. Elliott, Aine Slowey, Yulin Ye and Stuart J. Conway
Med. Chem. Commun., 2012
DOI: 10.1039/C2MD20079A