Sixteen novel and four known(4a, 4d, 4e, 4h) amine derivatives of furocoumarin were synthesized, then submitted to evaluation as stimulators of melanogenesis and tyrosinase in B16 murine cells. Among them, five compounds(4g, 4j-4m) showed potent activating effect on both melanogenesis and tyrosinase in vitro compared with positive control(8-MOP), the most widely used drugs for vitiligo in clinic. Noticeably, compounds 4h and 4j, which contain morpholine and piperazine, were recognized as the most effective stimulator of melanogenesis and tyrosianse in B16 cells separately. These derivatives may serve as lead compounds for further drug discovery for the treatment of vitiligo.