This study was carried out to discriminate the effects of the ramie leaf according to the drying methods (hot air drying and freeze drying) on antioxidative activity in vitro and antiproliferation in human cancer cells. There were no significant differences in total polyphenol content of ramie leaf ethanol extracts depending on the drying methods, but total flavonoid content was significantly higher in hot air dried ramie leaf (HR) than in freeze dried ramie leaf (FR). The DPPH radical scavenging activity of HR and FR ethanol extracts were found to be 77.74%, and 77.29% in 1000 ppm, respectively. Antioxidative index of HR and FR ethanol extracts measured by Rancimat were lower than those in BHT, BHA, and ascorbic acid, but were higher than that in control. The antiproliferation effect of 80% ethanol extracts of HR and FR on liver cancer cell line (H460), stomach cancer cell line (AGS), and lung cancer cell line (A549) were increased with a dose-dependent manner. The cancer cell growth inhibition activities of HR and FR ethanol extracts at the concentration of 800 μg/mL showed greater than 80% on Hep G2 and A549 cell line, and greater than 75% on AGS cell line. These results suggest that HR and FR ethanol extracts possess potential antioxidative effect and antiproliferation in human cancer cells, and those activities of ramie leaf ethanol extracts depending on the drying methods were similar.