The acquirement and mortality rate of cancer have been the global healthy problem, and attracted many resources from the academic and practical area try to find out the best therapeutic or alleviation way for the cancer. The unbalance of relationship between cell proliferation and apoptosis has been verified by many references that there is a closed linkage to the cancer. That is why people want to get the phytochemicals from some of vegetables and fruits, and avoid the inappropriate cell proliferation. Indole-3-carbinol is a product of the autolysis of glucosinolates present in the species of the genus Brassica. Now, a series of novel indole-3-carbinol derivatives have been synthesized, and studied the anti-cancer activity which including cytotoxic screen, cell cycle assay. Meanwhile, the pharmacological study will be undertaken to establish the mechanisms of action of these compounds.