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The antiproliferative activities of the new hybrids were evaluated against eight cancer cell lines using the sulforhodamine B assay. The most potent compound (<jats:bold>24b<\/jats:bold>) possessed high selectivity on the tested cell lines in the low micromolar range, with much lower effects on normal fibroblast cells (IC<jats:sub>50<\/jats:sub> &gt; 50\u2009\u00b5M). The cell lines derived from leukemia (Jurkat), cervix (HeLa), and colon (HCT116) cancers appeared to be the most sensitive, with IC<jats:sub>50<\/jats:sub> of 2\u2009\u00b5M. <jats:bold>24b<\/jats:bold> is the <jats:italic>N<\/jats:italic>\u2010ethylamide derivative with <jats:italic>p<\/jats:italic>\u2010dimethylaminobenzylidene at position 5 of the 4\u2010thiazolinone moiety. Other <jats:italic>N<\/jats:italic>\u2010substituents or arylidene derivatives showed lower activity. Hybrids with salicylamides showed lower activity than with methyl salicylate. The results clearly show that the modifications of the carboxy group and arylidene moiety greatly affect the activity. Investigating the possible molecular mechanisms of these hybrids revealed that they act through cell\u2010cycle arrest and induction of apoptosis and epidermal growth factor receptor (EGFR) inhibition. Molecular docking studies rationalize the molecular interactions of <jats:bold>24b<\/jats:bold> with EGFR. This work expands our knowledge of the structural requirements to improve the anticancer activity of 5\u2010aminosalicylic\u2010thiazolinone hybrids and pave the way toward multitarget anticancer salicylates.<\/jats:p>","DOI":"10.1002\/ardp.202300315","type":"journal-article","created":{"date-parts":[[2023,8,8]],"date-time":"2023-08-08T10:02:13Z","timestamp":1691488933000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":5,"title":["The design, synthesis, biological evaluation, and molecular docking of new 5\u2010aminosalicylamide\u20104\u2010thiazolinone hybrids as anticancer agents"],"prefix":"10.1002","volume":"356","author":[{"given":"Shimaa A.","family":"Othman","sequence":"first","affiliation":[{"name":"Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy Assiut University Assiut Egypt"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ola F.","family":"Abou\u2010Ghadir","sequence":"additional","affiliation":[{"name":"Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy Assiut University Assiut Egypt"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Wafaa S.","family":"Ramadan","sequence":"additional","affiliation":[{"name":"Research Institute for Medical and Health Sciences and College of Pharmacy University of Sharjah Sharjah United Arab Emirates"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yaser A.","family":"Mostafa","sequence":"additional","affiliation":[{"name":"Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy Assiut University Assiut Egypt"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Raafat","family":"El\u2010Awady","sequence":"additional","affiliation":[{"name":"Research Institute for Medical and Health Sciences and College of Pharmacy University of Sharjah Sharjah United Arab Emirates"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-4474-9086","authenticated-orcid":false,"given":"Hajjaj H. 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