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Herein, we report a novel photoclick\u2010and\u2010release strategy for the co\u2010activation of carbon monoxide and a self\u2010reporter, carbonyl sulfide, or sulfonamide with fast reaction kinetics (<jats:italic>k<\/jats:italic>: 1.4\u201322.6\u2005M<jats:sup>\u22121<\/jats:sup>\u2009s<jats:sup>\u22121<\/jats:sup>). Such a photoclick\u2010and\u2010release strategy was successfully applied in live cells to deliver carbon monoxide and a fluorescent self\u2010reporter, both of which exhibited pronounced antiproliferative activity against 4T1 cancer cells. It is conceivable that this photoclick\u2010and\u2010release strategy could find applications in other fields, in which a controlled bond cleavage is preferred.<\/jats:p>","DOI":"10.1002\/cbic.202200506","type":"journal-article","created":{"date-parts":[[2022,11,30]],"date-time":"2022-11-30T23:44:04Z","timestamp":1669851844000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":25,"title":["Photoclick and Release: Co\u2010activation of Carbon Monoxide and a Fluorescent Self\u2010reporter, COS or Sulfonamide with Fast Kinetics"],"prefix":"10.1002","volume":"24","author":[{"given":"Miao","family":"Liu","sequence":"first","affiliation":[{"name":"College of Pharmaceutical Science, Soochow University  Suzhou Jiangsu 215021 P. R. 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