Editing the structure of molecules
Nina Notman meets the chemists expanding the toolbox of reactions capable of adding, deleting and switching single atoms in rings at the heart of organic molecules
The majority of small molecule drugs have at least one ring system in their structural core. Sometimes the rings have biological activity themselves but more often than not their primary role is to offer structural rigidity.
When shown the structure of a hit molecule, scientists can very rapidly draw up a wish list of analogues on paper that would be worth testing against the biological target. But whether medicinal chemists have the tools to make these molecules easily is a different matter.
Creating a new synthesis for each analogue from commercially available starting materials is both costly and time consuming. An alternative approach is to use the hit molecule as the starting point and then make controlled and precise edits to its structure.