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Synthesis and Bioactivity Evaluation of Novel Chlorogenic Acid Derivatives Containing Amide Group

??OBJECTIVE To design and synthesize a series of chlorogenic acid derivatives in order to improve the solubility and lipid-water partition coefficients of chlorogenic acid, and test the bioactiviteies of the target compounds. METHODS The target compounds were synthesized from chlorogenic acid by three-step reactions of hydroxyl protection, acylation, and deprotection. The anti-tumor activities of the compounds were evaluated against two different tumor cell lines by MTT assay, and the DPPH method was used to measure the antioxidant activities of the compounds. RESULTS Eight title compounds were prepared, the structures of the compounds were confirmed by IR and NMR. The MTT assay showed that the compounds exhibited certain antitumor activities and better antioxidant activities, and the activities against A-549 and SGC-7901 tumor cells and the scavenging ratio to DPPH?? were similar to those of chlorogenic acid. CONCLUSION Chlorogenic acid derivatives containing amide group still have antitumor and antioxidant activities.