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However, a lack of selectivity toward cancer cells and associated side effects with current treatment options has fueled continued efforts throughout the world to find better anticancer drugs. Over the past decades, copper\u2010containing compounds have shown excellent anticancer activity. Cu(II) complexes are well studied and show broad\u2010spectrum pharmacological activity. The redox activity of copper ions contributes to cytotoxic activity in combination with ligands that possess bioactivity. Binding of copper with various types of bidentate, tridentate, and tetradentate ligands can activate the processes of necrosis, apoptosis, and angiogenesis. Copper induces the formation of reactive oxygen species to cleave DNA. Similarly, light\u2010assisted excitation of Cu(II) complexes in the red region of the electromagnetic spectrum helps produce different reactive species, thereby inducing anticancer activity through a photodynamic mechanism. In general, in\u2005vivo and in\u2005vitro studies have demonstrated that the administration of copper ions is effective against various cancer cell lines. Herein we discuss the past ten years of research into copper complexes of terpyridine\u2010, 2,2\u2019\u2010bipyridine\u2010, and 1,10\u2010phenanthroline\u2010based ligands as potential anticancer agents. The aspects of chemotherapy by redox\u2010mediated pathways and photodynamic therapy using light\u2010assisted excitation are reviewed, with a focus on mechanisms of activity, details of important experimental procedures, as well as drawbacks in the design of copper\u2010containing drugs.<\/jats:p>","DOI":"10.1002\/cmdc.202200652","type":"journal-article","created":{"date-parts":[[2023,2,11]],"date-time":"2023-02-11T14:43:51Z","timestamp":1676126631000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":61,"title":["Recent Development of Copper (II) Complexes of Polypyridyl Ligands in Chemotherapy and Photodynamic Therapy"],"prefix":"10.1002","volume":"18","author":[{"given":"Jansi","family":"Rani J","sequence":"first","affiliation":[{"name":"Department of Chemistry School of Advanced Sciences Vellore Institute of Technology  Vellore 632014 India"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1658-5392","authenticated-orcid":false,"given":"Sovan","family":"Roy","sequence":"additional","affiliation":[{"name":"Department of Chemistry School of Advanced Sciences Vellore Institute of Technology  Vellore 632014 India"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2023,3,6]]},"reference":[{"key":"e_1_2_9_1_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ccr.2020.213339"},{"key":"e_1_2_9_2_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.cell.2011.02.013"},{"key":"e_1_2_9_3_1","unstructured":"World Health Organization WHO (July 12 2019) https:\/\/www.who.int\/health-topics\/cancer#tab=tab_1."},{"key":"e_1_2_9_4_1","unstructured":"National Cancer Institute (2019) https:\/\/www.cancer.gov\/about-cancer\/treatment\/types\/biomarker-testing-cancer-treatment."},{"key":"e_1_2_9_5_1","doi-asserted-by":"publisher","DOI":"10.1038\/205698a0"},{"key":"e_1_2_9_6_1","doi-asserted-by":"publisher","DOI":"10.1021\/ja9021717"},{"key":"e_1_2_9_7_1","doi-asserted-by":"publisher","DOI":"10.1038\/nrd1691"},{"key":"e_1_2_9_8_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ctrv.2006.09.006"},{"key":"e_1_2_9_9_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ccr.2018.12.007"},{"key":"e_1_2_9_10_1","doi-asserted-by":"publisher","DOI":"10.2174\/138161210791209009"},{"key":"e_1_2_9_11_1","doi-asserted-by":"publisher","DOI":"10.1021\/cr980419w"},{"key":"e_1_2_9_12_1","doi-asserted-by":"publisher","DOI":"10.1039\/B922209J"},{"key":"e_1_2_9_13_1","doi-asserted-by":"publisher","DOI":"10.1039\/b705551j"},{"key":"e_1_2_9_14_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.chemrev.8b00685"},{"key":"e_1_2_9_15_1","doi-asserted-by":"publisher","DOI":"10.1039\/b706075k"},{"key":"e_1_2_9_16_1","doi-asserted-by":"publisher","DOI":"10.1021\/cr900134a"},{"key":"e_1_2_9_17_1","doi-asserted-by":"publisher","DOI":"10.1126\/science.1083004"},{"key":"e_1_2_9_18_1","doi-asserted-by":"publisher","DOI":"10.1002\/ejic.201600908"},{"key":"e_1_2_9_19_1","doi-asserted-by":"publisher","DOI":"10.1158\/1535-7163.MCT-16-0445"},{"key":"e_1_2_9_20_1","doi-asserted-by":"publisher","DOI":"10.1039\/C6DT01738J"},{"key":"e_1_2_9_21_1","doi-asserted-by":"publisher","DOI":"10.1002\/chem.201503866"},{"key":"e_1_2_9_22_1","doi-asserted-by":"publisher","DOI":"10.1039\/C2DT32333H"},{"key":"e_1_2_9_23_1","doi-asserted-by":"publisher","DOI":"10.1021\/acs.inorgchem.6b00359"},{"key":"e_1_2_9_24_1","doi-asserted-by":"publisher","DOI":"10.1039\/D0DT02167A"},{"key":"e_1_2_9_25_1","doi-asserted-by":"publisher","DOI":"10.1021\/jacs.1c09010"},{"key":"e_1_2_9_26_1","doi-asserted-by":"publisher","DOI":"10.2147\/DDDT.S119488"},{"key":"e_1_2_9_27_1","doi-asserted-by":"crossref","unstructured":"R. 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