Although　photodynamic　therapy　has　been　extensively　studied　in　recent　years　and　preclinical　studies　have　shown　promising　results,　strategies　for　enhancing　PDT　outcomes　and　reducing　side　effects　still　urgently　need　to　be　developed.　In　this　study,　a　series　of　Tamoxifen-zinc(II)　phthalocyanine　conjugates　have　been　designed　and　synthesized.　In　these　＂double-headed＂　conjugates,　photodynamic　therapy　agent　zinc(II)　phthalocyanine　and　hormone　therapy　drug　Tamoxifen　were　combined　via　oligoethylene　glycol　linkers.　The　conjugates　show　high　specificity,　and　some　of　them　show　cytotoxic　effects　against　the　MCF-7　cells　overexpressed　Estrogen　receptor,　due　to　the　targeting　and　cytostatic　Tamoxifen　moiety.　Upon　illumination,　all　these　conjugates　show　high　cytotoxicity　due　to　the　photosensitizing　phthalocyanine　unit.　Their　structure-activity　relationship　was　also　assessed.　The　results　show　that　α-substituted　Tamoxifen-zinc(II)　phthalocyanine　conjugates　are　highly　promising　anticancer　targeting　agents　which　exhibit　additive　effects　of　photodynamic　therapy　and　hormone　therapy.　©　2019　World　Scientific　Publishing　Company.