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Resveratrol is a well-known natural antioxidant and cancer chemopreventive agent that has attracted much interest in the past decade. Resveratrol-directed compounds were synthesized, and their antioxidant effects against reactive oxygen species (ROS)-induced DNA damage, their prooxidant effects on DNA damage in the presence cupric ions, and their cytotoxic and apoptosis-inducing effects on human promyelocytic leukemia (HL-60) cells were investigated in vitro. It was found that the compounds bearing o-diphenoxyl groups exhibited remarkably higher activities in inhibiting ROS-induced DNA damage, accelerating DNA damage in the presence cupric ions, and inducing apoptosis of HL-60 cells compared with the ones bearing no such groups. The detail mechanism of the structure−activity relationship was also studied by the oxidative product analysis of resveratrol and its analogues with galvinoxyl radical or cupric ions and UV−visible spectra change in the presence cupric ions. This study reveals a good and interesting correlation between antioxidant and prooxidant activity, as well as cytotoxicity and apoptosis-inducing activity against HL-60 cells, and provides an idea for designing antioxidant-based cancer chemoprevention agents. [ABSTRACT FROM AUTHOR]

Pseudolaric acid B (PAB), discovered as a promising angiogensis inhibitor, was served as the anticancer drug lead, and a series of its derivatives were synthesized. Among them, some derivatives, such as 13c− 13k, exhibited potent inhibition on the HMEC-1 cell proliferation and strong cytotoxic activities against the tested six tumor cell lines. The PAB derivatives 13c− 13kalso showed significant and specific inhibition on HMEC-1 cell migration in vitro, and only 13dexpressed moderate activity against HMEC-1 cell tube formation. The in vitro anticancer tests of the selected natural PAB analogs and the structurally modified PAB derivatives have led to the establishment of a clear structure–activity relationship. [ABSTRACT FROM AUTHOR]