The　combination　of　photodynamic　therapy　and　chemotherapy　is　a　promising　strategy　to　overcome　growing　problems　in　contemporary　medicine,　such　as　low　therapeutic　efficacy　and　drug　resistance.　Four　zinc(II)　phthalocyanine-coumarin　conjugates　were　synthesized　and　characterized.　In　these　complexes,　zinc(II)　phthalocyanine　was　used　as　the　photosensitizing　unit,　and　a　coumarin　derivative　was　selected　as　the　cytostatic　moiety;　the　two　components　were　linked　via　a　tri(ethylene　glycol)　chain.　These　conjugates　exhibit　high　photocytotoxicity　against　HepG2　human　hepatocarcinoma　cells,　with　low　IC50　values　in　the　range　of　0.014-0.044　mu　m.　The　high　photodynamic　activities　of　these　conjugates　are　in　accordance　with　their　low　aggregation　tendency　and　high　cellular　uptake.　One　of　these　conjugates　exhibits　high　photocytotoxicity　and　significantly　higher　chemocytotoxicity.　The　results　clearly　show　that　the　two　antitumor　components　in　these　conjugates　work　in　a　cooperative　fashion.　As　shown　by　confocal　microscopy,　the　conjugates　can　localize　in　the　mitochondria　and　lysosomes,　and　one　of　the　conjugates　can　also　localize　in　the　cell　nuclei.