Abstract: In order to discover compounds with better biological activity, a series of furazan derivatives were synthesized based on the structural modification of INCB024360 (Epacadostat). The anti-proliferative activities of new synthesized compounds 4a–o were screened in vitro against a panel of four human solid tumor cell lines (HepG2; A549, Hela and A375). We also reported the toxicity of compounds with low IC50 values on human hepatic cell line (LO2), and the apoptosis effect of compounds 4h and 4i on Hela cell. The results showed that several compounds displayed good inhibitory activity, even better than the positive compound 5-fluorouracil (5-FU) for specific cell lines. In addition, the toxicity of compounds 4h–j and 4m–o towards LO2 were lower than the positive compound 5-FU.