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However, MOF\u2010based drug carriers with active tumor\u2010targeting function have not been extensively researched until now. Here we show a strategy for constructing active tumor\u2010targeted NMOF drug carriers by anchoring functional folic acid (FA) molecules onto the metal clusters of NMOFs. Two zirconium\u2010based MOFs, MOF\u2010808 and NH<jats:sub>2<\/jats:sub>\u2010UiO\u201066, were chosen as models to reduce to the nanoscale for application as drug carriers, and then the terminal carboxylates of FA molecules were coordinated to Zr<jats:sub>6<\/jats:sub> clusters on the surfaces of the nanoparticles by substitution of the original formate or terminal \u2010OH ligands. The successful modification with FA was confirmed by solid\u2010state <jats:sup>13<\/jats:sup>C MAS NMR and UV\/Vis spectroscopy and other characterization methods. Drug loading and controlled release behavior at different pH were determined by utilizing the anticancer drug 5\u2010fluorouracil (5\u2010FU) as the model drug. Confocal laser scanning microscopy measurements further demonstrated that 5\u2010FU\u2010loaded FA\u2010NMOFs have excellent targeting ability through the efficient cellular uptake of FA\u2010NMOFs. This work opens up a new avenue to the construction of active tumor\u2010targeted NMOF\u2010based drug carriers with potential for cancer therapies.<\/jats:p>","DOI":"10.1002\/chem.201804153","type":"journal-article","created":{"date-parts":[[2018,8,20]],"date-time":"2018-08-20T04:17:17Z","timestamp":1534738637000},"page":"17148-17154","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":124,"title":["Folic Acid Functionalized Zirconium\u2010Based Metal\u2013Organic Frameworks as Drug Carriers for Active Tumor\u2010Targeted Drug Delivery"],"prefix":"10.1002","volume":"24","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-5839-7846","authenticated-orcid":false,"given":"Hong","family":"Dong","sequence":"first","affiliation":[{"name":"School of Materials Science and Engineering College of Chemical and Environmental Engineering Harbin University of Science and Technology  Harbin 150040 P.\u2005R. 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