Symmetrical and un-symmetrical curcumin analogues as selective COX-1 and COX-2 inhibitor

Curcumin, a popular herbal medicine derived from turmeric, blocks the synthesis of prostaglandins by inhibiting Cyclooxygenase-1 and 2 (COX-1 and COX2). We have recently reported an efficient method of synthesizing curcumin and synthesised analogues. In the present study, we have investigated sixteen novel analogues of curcumin for their ability to inhibit COX-1 and COX-2. We report here that most of the curcumin analogues display selective inhibition of COX-2, whereas a few suppress COX-1 activity. Further, we examined the binding of these inhibitors by molecular docking and observed that the compound with pronounced selectivity for COX-2 displayed better binding to COX-2 compared to curcumin.

Automated summary

In this study, sixteen novel analogues of curcumin were investigated for their inhibition of COX-1 and COX-2. Most analogues displayed selective inhibition of COX-2, while a few suppressed COX-1 activity. Molecular docking analysis showed that compounds with pronounced selectivity for COX-2 exhibited better binding to COX-2 compared to curcumin.