A Tale of Drug Discovery: Synthesis, Bioassay, and Computational Docking Studies of Novel Curcuminoids

Abstract With the goal to overcome the bio-physicochemical drawbacks of parent curcumin (CUR) and to develop analogues with improved biological profiles and higher potencies, the present account provides a review summary of the work in my laboratory on the synthesis of structurally diverse libraries of curcuminoids (CURs), their in vitro bioassays, and computational docking studies. These efforts resulted in the discovery of a subset of compounds with exceptional antiproliferative and apoptotic activity that warrant further investigation. 1 Introduction 2 Synthetic Strategies 3 Bioassay Studies 4 Computational Docking Studies 5 Summary and Outlook