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Twelve of the obtained compounds were evaluated for their in vitro cytotoxic activity against 60 different human cancer cell lines according to the National Cancer Institute protocol. Among the screened compounds, the symmetrical <jats:italic>N<\/jats:italic>\u2010butyl <jats:italic>bis<\/jats:italic>\u2010quinolinyl\u2010chalcone <jats:bold>14g<\/jats:bold> and the unsymmetrical quinolinyl\u2010<jats:italic>bis<\/jats:italic>\u2010chalcone <jats:bold>17o<\/jats:bold> bearing a 7\u2010chloro\u2010substitution on the <jats:italic>N<\/jats:italic>\u2010benzylquinoline moiety and 4\u2010hydroxy\u20103\u2010methoxy substituent on the phenyl ring, respectively, exhibited the highest overall cytotoxicity against the evaluated cell lines with a GI<jats:sub>50<\/jats:sub> range of 0.16\u20135.45\u2009\u00b5M, with HCT\u2010116 (GI<jats:sub>50<\/jats:sub>\u2009=\u20090.16) and HT29 (GI<jats:sub>50<\/jats:sub>\u2009=\u20090.42\u2009\u03bcM) (colon cancer) representing best\u2010case scenarios. Notably, several GI<jats:sub>50<\/jats:sub> values for these compounds were lower than those of the reference drugs doxorubicin and 5\u2010FU. Docking studies performed on selected derivatives yielded very good binding energies in the active site of proteins that participate in key carcinogenic pathways.<\/jats:p>","DOI":"10.1002\/ardp.202100094","type":"journal-article","created":{"date-parts":[[2021,5,29]],"date-time":"2021-05-29T14:49:59Z","timestamp":1622299799000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":14,"title":["Design, synthesis, and molecular docking study of novel quinoline\u2010based <i>bis<\/i>\u2010chalcones as potential antitumor agents"],"prefix":"10.1002","volume":"354","author":[{"given":"Daniel","family":"Insuasty","sequence":"first","affiliation":[{"name":"Departamento de Qu\u00edmica y Biolog\u00eda, Divisi\u00f3n de Ciencias B\u00e1sicas Universidad del Norte  Barranquilla Colombia"},{"name":"Department of Chemistry, Research Group of Heterocyclic Compounds Universidad del Valle  Cali 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