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Most of the enamine derivatives with IC<jats:sub>50<\/jats:sub>values of 86\u2013168\u2005\u03bcM demonstrated much stronger antiproliferative activity than the starting molecules against the cancer cells. While, among the enamine derivatives, four compounds displayed higher cytotoxic potency than the control drugs (5\u2010fluorouracil and cisplatin) against the Hep3B cell lines, these compounds did not exhibit any significant toxicity against normal cells, FL. The UV\/VIS spectral data suggest that eight compounds cause hypochromism with a slight bathochromic shift (\u223c6\u2005nm), indicating that they bind to the DNA by way of an intercalative or minor groove binding mode. The binding constants of the compounds are in the range of 0.1\u00d7103\u2005M<jats:sup>\u22121<\/jats:sup>\u20132.3\u00d7104\u2005M<jats:sup>\u22121<\/jats:sup>. The antiproliferative activity of studied enamine derivatives could possibly be due to their DNA binding as well as their cytotoxic properties. In addition to these assays, the chalcones and enamine derivatives were investigated by molecular docking to calculate the synergistic effect of antiproliferative activities against six human cancer cell lines.<\/jats:p>","DOI":"10.1002\/cbdv.202000139","type":"journal-article","created":{"date-parts":[[2020,5,6]],"date-time":"2020-05-06T19:01:58Z","timestamp":1588791718000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":14,"title":["Synthesis, Antiproliferative and Cytotoxic Activities, DNA Binding Features and Molecular Docking Study of Novel Enamine Derivatives"],"prefix":"10.1002","volume":"17","author":[{"given":"Meliha","family":"Burcu G\u00fcrdere","sequence":"first","affiliation":[{"name":"Department of Chemistry Faculty of Arts and Sciences Tokat Gaziosmanpa\u015fa University 60250 Tokat Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ali","family":"Aydin","sequence":"additional","affiliation":[{"name":"Department of Basic Medical Science Faculty of Medicine Yozgat Bozok University 66100 Yozgat Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Belk\u0131z","family":"Yencilek","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Arts and Sciences Tokat Gaziosmanpa\u015fa University 60250 Tokat Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fatih","family":"Ert\u00fcrk","sequence":"additional","affiliation":[{"name":"Vocational School Occupational Health and Safety Program Istanbul Arel University 34100 Istanbul Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"O\u011fuz","family":"\u00d6zbek","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Arts and Sciences Tokat Gaziosmanpa\u015fa University 60250 Tokat Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sultan","family":"Erkan","sequence":"additional","affiliation":[{"name":"Chemistry and Chemical Processing Technologies Y\u0131ld\u0131zeli Vocational School Sivas Cumhuriyet University 58140 Sivas Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yakup","family":"Budak","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Arts and Sciences Tokat Gaziosmanpa\u015fa University 60250 Tokat Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mustafa","family":"Ceylan","sequence":"additional","affiliation":[{"name":"Department of Chemistry Faculty of Arts and Sciences Tokat Gaziosmanpa\u015fa University 60250 Tokat Turkey"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2020,6,25]]},"reference":[{"key":"e_1_2_7_1_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2017.12.040"},{"key":"e_1_2_7_2_1","unstructured":"Cancer Fact Sheet Feb. 2017 World Health Organisation 2017."},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.canlet.2013.09.016"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1039\/C4NJ00936C"},{"key":"e_1_2_7_5_1","first-page":"21","article-title":"\u2018Recent advancements in 1,4-disubstituted 1H-1,2,3-triazoles as potential anticancer agents\u2019","volume":"18","author":"Lal K.","year":"2018","journal-title":"ACS Med. 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