This study aims at developing new organoselenium compounds with good anticancer ability and low biotoxicity. Sucrose selenious ester (sucrose-Se) was synthesized by the reaction between sucrose and selenium oxychloride. MTT assay showed that sucrose-Se effectively inhibited the proliferation of cervical cancer cell line HeLa in a dose-dependent manner without cytostatic influence on human normal liver cell line HL-7702. Morphological observation and agarose gel electrophoresis demonstrated that sucrose-Se induced apoptosis to HeLa cells. In addition, sucrose-Se was able to inhibit proliferation of bladder carcinoma cell line 5637, human malignant melanoma cell line A375, and gastric carcinoma cell line MGC-803. Median lethal dose of sucrose-Se and sodium selenite was 290.0 and 13.1 ppm, respectively, in the acute toxicity test on mice. In conclusion, sucrose-Se has potential in cancer chemoprevention due its apoptosis induction capacity and low biotoxicity.