A folate-porphyrin conjugate 1 has been synthesized and characterized. The cellular uptake of conjugate I by Hela cells was about 35 times higher than that of precursor porphyrin 3 after 24h of incubation and can be inhibited competitively by free folic acid. Moreover, conjugate I exhibited much lower dark cytotoxicity against Hela cells in vitro but significant photocytotoxicity with 86.4% cell growth inhibition ratio after irradiation.