A　unique　zirconium-based　framework　named　N3-UiO-66-NH2,　which　can　be　used　as　a　fabricated　material　to　achieve　the　dual　functional　chemical　modification　of　UiO-66,　was　synthesized　and　demonstrated.　This　work　offers　a　facile　and　selective　covalent　post-synthetic　modification　of　UiO-66　by　different　chemical　reactions　related　to　azide-　and　amino-groups,　respectively.　Using　N3-UiO-66-NH2　as　a　fabricated　material,　a　newly　dual　functionalized　MOF　named　E-UiO-66-Pc,　in　which　a　carboxyl　substituted　zinc　phthalocyanine　(Pc)　and　Erlotinib　(E)　were　employed　as　a　photosensitizer　and　targeting　moiety,　was　designed　and　synthesized　via　amidation　and　click　chemistry,　respectively.　The　photochemical　properties,　tumor　specificity　and　anticancer　activity　of　E-UiO-66-Pc　were　investigated.　We　further　demonstrated　that　it　is　viable　to　achieve　facile　and　selective　covalent　post-synthetic　modification　of　N3-UiO-66-NH2　with　Pc　and　E　and　obtained　a　series　of　functionalized　UiO-66　nanomaterials.　The　Pc-containing　UiO-66　nanomaterials　exhibit　high　photodynamic　activity,　and　the　Erlotinib-containing　UiO-66　nanomaterials　show　obvious　dark　cytotoxicity　and　high　selective　affinity　to　cancer　cells.　E-UiO-66-Pc　reveals　cooperative　photodynamic　and　targeted　anticancer　activity.　To　the　best　of　our　knowledge,　this　is　the　only　example　of　UiO-66　with　two　different　chemical　handles　(-NH2　and　-N3)　anchoring　to　different　functional　molecules　via　amidation　and　click　chemistry,　respectively.　©　2017　The　Royal　Society　of　Chemistry.