Synthesis, and antioxidant, thrombin-inhibitory, and anticancer activities of hydroxybenzamide derivatives

Abstract

Four hydroxybenzamide derivatives were synthesized from protocatechuic acid. The antioxidant activities of these derivatives were evaluated in vitro using DPPH radical scavenging and reducing power assays. In addition, these compounds were subjected to a chromogenic thrombin-inhibitory assay using Chromozym-TH as the substrate. The anticancer effects of these derivatives were also investigated using the MTT assay in three human cancer cell lines. Four derivatives exhibited excellent DPPH radical scavenging activity and redox potential. Their highly inhibitory effect against thrombin may allow them to be utilized as novel micromolecule thrombin inhibitors. Furthermore, four derivatives demonstrated different inhibitory activities in three human cancer cell lines but showed minimal harmful effects on normal HUVEC cells. Therefore, hydroxybenzamide derivatives indicate the superior antioxidant, thrombin-inhibitory, and anticancer activities along with the excellent biocompatibility, which have the potential application in therapeutic interventions and disease prevention of cancer, thrombotic diseases, and aging.