The chemistry of the Sarco/Endoplasmic Calcium-ATPase (SERCA) inhibitor thapsigargin has been developed enabling selective transformation of the functional groups in the molecule. Appropriate substitutions of the side chains are performed with the purpose of generating analogues, which can be used as drugs or diagnostics. The developed pharmacophore model is improved by structure activity relationship. The structure activity studies will be complemented with computational chemistry in order to design a SERCA inhibitor possessing a simple skeleton.

This project is a part of the SPOTLight programme.