| Currently,natural products are still deemed as lead templates for the design and discovery of drugs.Resveratrol,which was first discovered in,has been extensively investigated as anti-aging,anti-oxidative,anticancer,anti-inflammatory,treatment of type II diabetes and cardiovascular agents.Based on our previous researches,series of novel resveratrol hybrids were reported with significant anti-inflammatory and antitumor activities.As a part of our continuous interest in search of active natural analogs with anti-inflammatory and antitumor activities,we synthesized and evaluated the biological activities of these resveratrol-based derivatives.(1)Twenty-two novel resveratrol-based flavone derivatives were synthesized.The effect of compounds on inflammatory cytokines expression were evaluated by Elisa and Griess method.Among them,compound H5 was found to be the most potent one in inhibiting NO,TNF-α and IL-6 production.Further study indicated that compound H5 could suppress THE expression of proteins i NOS,COX-2 through regulating TLR4 to blocking-up the NF-κB/MAPKs signaling pathway.(2)Twenty-three novel resveratrol-based nitrovinylstilbenes derivatives were synthesized.Antitumor activity evaluations of the derivatives were performed in the MGC803 and SMMC-7721 cell lines by using the MTT assay.The results indicated that most compounds exhibited good to significant antitumor activity.Compound Z15 showed the best antitumor activity against the MGC803 and SMMC-7721 with the IC50 values of 3.31 μM and 2.5 μM,respectively.In summary,the compounds of H5,Z15 were screened out.Based on the SAR studies result,it provided more information for searching novel therapeutic agents for future. |
