Two　novel　glucosylated　zinc(II)　phthalocyanines　7a-7b,　as　well　as　the　acetyl-protected　counterparts　6a-6b,　have　been　synthesized　by　the　Cu(I)-catalyzed　1,3-dipolar　cycloaddition　between　the　propargylated　phthalocyanine　and　azide-substituted　glucoses.　All　of　these　phthalocyanines　were　characterized　with　various　spectroscopic　methods　and　studied　for　their　photo-physical,　photo-chemical,　and　photo-biological　properties.　With　glucose　as　the　targeting　unit,　phthalocyanines　7a-7b　exhibit　a　specific　affinity　to　MCF-7　breast　cancer　cells　over　human　embryonic　lung　fibroblast　(HELF)　cells,　showing　higher　cellular　uptake.　Upon　illumination,　both　photosensitizers　show　high　cytotoxicity　with　IC50　as　low　as　0.032　mu　M　toward　MCF-7　cells,　which　are　attributed　to　their　high　cellular　uptake　and　low　aggregation　tendency　in　the　biological　media,　promoting　the　generation　of　intracellular　reactive　oxygen　species　(ROS).　Confocal　laser　fluorescence　microscopic　studies　have　also　revealed　that　they　have　high　and　selective　affinities　to　the　lysosomes,　but　not　the　mitochondria,　of　MCF-7　cells.　The　results　show　that　these　two　glucosylated　zinc(II)　phthalocyanines　are　potential　anticancer　agents　for　targeting　photodynamic　therapy.