{Reference Type}: Journal Article
{Title}: Synthesis, biological evaluation and docking studies of N-substituted resveratrol derivatives.
{Author}: Wu H;Liu L;Song M;Yin X;Chen M;Lv G;Zhao F;Mou X;
{Journal}: Fitoterapia
{Volume}: 174
{Issue}: 0
{Year}: 2024 Apr 28
{Factor}: 3.204
{DOI}: 10.1016/j.fitote.2024.105872
{Abstract}: A total of 19 resveratrol derivatives, including 12 imines and 7 amines, were synthesized, among which compounds 1, 5, 6, 7', 11', and 13 are new compounds. The anti-inflammatory and antitumor activities of these compounds were evaluated in vitro. The results revealed that compounds 1, 6, 8', 12, and 12' exhibited significant inhibitory effects (> 50%) on NO production at the concentration of 10 μM and their NO production inhibitory activities have a significant concentration-dependent ability. Additionally, compounds 8' and 12' showed promising COX-2 inhibitory activity, and the molecular docking analysis indicated their stable binding to multiple amino acid residues within the active pocket of COX-2 through hydrogen bonding. Moreover, compound 12' exhibited inhibitory effects on various tumor cell lines and induced apoptosis in MCF-7 breast cancer cells, which was not observed with resveratrol alone. Therefore, the N-substituted structural modification of resveratrol would have possibly enhanced the bioactivity of resveratrol and facilitated its application.