Despite a huge body of research in the past two decades investigating the antioxidant, antiinflammatory,
anti-microbial, and anti-carcinogenic properties of curcumin (CUR), a CUR-based antitumor
drug is yet to be developed. Lack of success in achieving this goal stems from CUR’s unfavorable
biophysicochemical features, particularly poor solubility, low bioavailability, and rapid metabolism,
coupled with a complex biological profile making it difficult to determine its mechanism of action.
A significant body of literature aimed at improving its physicochemical properties through synthesis
or by designing delivery methods has been published, and the progress in these areas has been
reviewed. The present review aims to summarize recent progress in the synthesis of structurally diverse
“curcumin-inspired” compounds along with computational docking and bioassay studies,
through which a number of promising analogs have been identified that warrant further study.