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Four compounds, <jats:bold>3a<\/jats:bold>, <jats:bold>3c<\/jats:bold>, <jats:bold>5b<\/jats:bold>, and <jats:bold>5c<\/jats:bold>, showed 1.4\u20139.2\u2010fold more potent anticancer activity than celecoxib. The antiproliferative activity of the most potent compounds, <jats:bold>3c<\/jats:bold>, <jats:bold>5b<\/jats:bold>, and <jats:bold>5c<\/jats:bold>, seems to be associated well with their ability to induce apoptosis in MCF\u20107 cells (18\u201324\u2010fold). This evidence was supported by an increase in the expression of the tumor suppressor gene p53 (4\u20136\u2010fold), the elevation in the Bax\/BCL\u20102 ratio, and a significant increase in the level of active caspase\u20107 (4\u20137\u2010fold). Moreover, compounds <jats:bold>3c<\/jats:bold> and <jats:bold>5c<\/jats:bold> showed significant cyclooxygenase\u20102 (COX\u20102) inhibitory activity. They were also docked into the crystal structure of the COX\u20102 enzyme (PDB ID: 3LN1) to understand their mode of binding.<\/jats:p>","DOI":"10.1002\/ardp.202200190","type":"journal-article","created":{"date-parts":[[2022,8,17]],"date-time":"2022-08-17T14:13:53Z","timestamp":1660745633000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":12,"title":["Design, synthesis, and biological evaluation of new celecoxib analogs as apoptosis inducers and cyclooxygenase\u20102 inhibitors"],"prefix":"10.1002","volume":"355","author":[{"given":"Eman F.","family":"Abdelhaleem","sequence":"first","affiliation":[{"name":"Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy Cairo University  Cairo Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6091-829X","authenticated-orcid":false,"given":"Asmaa E.","family":"Kassab","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy Cairo University  Cairo Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hala B.","family":"El\u2010Nassan","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy Cairo University  Cairo Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Omneya M.","family":"Khalil","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy Cairo University  Cairo Egypt"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2022,8,17]]},"reference":[{"key":"e_1_2_7_2_1","doi-asserted-by":"publisher","DOI":"10.3322\/caac.21660"},{"key":"e_1_2_7_3_1","doi-asserted-by":"publisher","DOI":"10.1002\/smll.202004258"},{"key":"e_1_2_7_4_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.msec.2021.112024"},{"key":"e_1_2_7_5_1","doi-asserted-by":"publisher","DOI":"10.1002\/ardp.202100368"},{"key":"e_1_2_7_6_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.yane.2012.02.046"},{"key":"e_1_2_7_7_1","doi-asserted-by":"publisher","DOI":"10.5306\/wjco.v5.i4.677"},{"key":"e_1_2_7_8_1","doi-asserted-by":"publisher","DOI":"10.1097\/MD.0000000000022544"},{"key":"e_1_2_7_9_1","doi-asserted-by":"publisher","DOI":"10.1007\/bf00686511"},{"key":"e_1_2_7_10_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.jdsr.2007.10.003"},{"key":"e_1_2_7_11_1","doi-asserted-by":"publisher","DOI":"10.1016\/S0140-6736(05)75961-4"},{"key":"e_1_2_7_12_1","doi-asserted-by":"publisher","DOI":"10.1055\/s-2001-12868"},{"key":"e_1_2_7_13_1","doi-asserted-by":"publisher","DOI":"10.1080\/13543776.2019.1623880"},{"key":"e_1_2_7_14_1","doi-asserted-by":"publisher","DOI":"10.4137\/bcbcr.s2291"},{"key":"e_1_2_7_15_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.taap.2011.06.019"},{"key":"e_1_2_7_16_1","doi-asserted-by":"publisher","DOI":"10.1186\/1475-2867-12-53"},{"key":"e_1_2_7_17_1","doi-asserted-by":"publisher","DOI":"10.3906\/biy-1703-101"},{"key":"e_1_2_7_18_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.cdp.2003.12.005"},{"key":"e_1_2_7_19_1","doi-asserted-by":"publisher","DOI":"10.1002\/ijc.20639"},{"key":"e_1_2_7_20_1","doi-asserted-by":"publisher","DOI":"10.1517\/13543784.17.2.197"},{"key":"e_1_2_7_21_1","doi-asserted-by":"publisher","DOI":"10.1023\/A:1025863029529"},{"key":"e_1_2_7_22_1","doi-asserted-by":"publisher","DOI":"10.2147\/CMAR.S178567"},{"key":"e_1_2_7_23_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.canlet.2011.01.012"},{"key":"e_1_2_7_24_1","doi-asserted-by":"publisher","DOI":"10.1038\/onc.2015.349"},{"key":"e_1_2_7_25_1","doi-asserted-by":"publisher","DOI":"10.2174\/1381612043453108"},{"key":"e_1_2_7_26_1","doi-asserted-by":"publisher","DOI":"10.4155\/fmc.11.177"},{"key":"e_1_2_7_27_1","doi-asserted-by":"publisher","DOI":"10.1002\/ijc.25033"},{"key":"e_1_2_7_28_1","doi-asserted-by":"publisher","DOI":"10.1093\/jnci\/94.23.1745"},{"key":"e_1_2_7_29_1","doi-asserted-by":"publisher","DOI":"10.1038\/s41420-018-0120-z"},{"key":"e_1_2_7_30_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2019.01.016"},{"key":"e_1_2_7_31_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2018.07.024"},{"key":"e_1_2_7_32_1","doi-asserted-by":"publisher","DOI":"10.1016\/j.bioorg.2020.104369"},{"key":"e_1_2_7_33_1","doi-asserted-by":"crossref","unstructured":"A. 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