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Using a specific NAMPT activity assay, up to an 18\u2010fold increase in inhibition potency was measured upon red\u2010light activation of [<jats:bold>2<\/jats:bold>]Cl<jats:sub>2<\/jats:sub>, while [<jats:bold>1<\/jats:bold>]Cl<jats:sub>2<\/jats:sub> was thermally unstable. For the first time, the dark and red\u2010light\u2010induced cytotoxicity of these photocaged compounds could be tested under hypoxia (1\u2009% O<jats:sub>2<\/jats:sub>). In skin (A431) and lung (A549) cancer cells, a 3\u2010 to 4\u2010fold increase in cytotoxicity was found upon red\u2010light irradiation for [<jats:bold>2<\/jats:bold>]Cl<jats:sub>2<\/jats:sub>, whether the cells were cultured and irradiated with 1\u2009% or 21\u2009% O<jats:sub>2<\/jats:sub>. These results demonstrate the potential of photoactivated chemotherapy for hypoxic cancer cells, in which classical photodynamic therapy, which relies on oxygen activation, is poorly efficient.<\/jats:p>","DOI":"10.1002\/anie.201703890","type":"journal-article","created":{"date-parts":[[2017,6,30]],"date-time":"2017-06-30T18:06:34Z","timestamp":1498845994000},"page":"11549-11553","source":"Crossref","is-referenced-by-count":205,"title":["A Red\u2010Light\u2010Activated Ruthenium\u2010Caged NAMPT Inhibitor Remains Phototoxic in Hypoxic Cancer Cells"],"prefix":"10.1002","volume":"56","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-2841-4742","authenticated-orcid":false,"given":"Lucien N.","family":"Lameijer","sequence":"first","affiliation":[{"name":"Leiden Institute of Chemistry Leiden University Gorlaeus Laboratories  P.O Box 9502 2300 RA Leiden The Netherlands"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dani\u00ebl","family":"Ernst","sequence":"additional","affiliation":[{"name":"Leiden Institute of Chemistry Leiden University Gorlaeus Laboratories  P.O Box 9502 2300 RA Leiden The Netherlands"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-8793-4540","authenticated-orcid":false,"given":"Samantha L.","family":"Hopkins","sequence":"additional","affiliation":[{"name":"Leiden Institute of Chemistry Leiden University Gorlaeus Laboratories  P.O Box 9502 2300 RA Leiden The Netherlands"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Michael S.","family":"Meijer","sequence":"additional","affiliation":[{"name":"Leiden Institute of Chemistry Leiden University Gorlaeus Laboratories  P.O Box 9502 2300 RA Leiden The Netherlands"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-6538-3645","authenticated-orcid":false,"given":"Sven H. 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