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All tested compounds showed a dual antagonist profile on both PPAR subtypes; based on transactivation results, seven compounds were selected to test their in vitro antiproliferative activity in a panel of eight cancer cell lines with different expression rates of PPAR\u03b1 and PPAR\u03b3. <jats:bold>3f<\/jats:bold> was identified as the most cytotoxic compound, with higher potency in the colorectal cancer cell lines HT\u201029 and HCT116. Compound <jats:bold>3f<\/jats:bold> induced a concentration\u2010dependent activation of caspases and cell\u2010cycle arrest in both colorectal cancer models. Docking experiments were also performed to shed light on the putative binding mode of this novel class of dual PPAR\u03b1\/\u03b3 antagonists.<\/jats:p>","DOI":"10.1002\/ardp.202400086","type":"journal-article","created":{"date-parts":[[2024,5,29]],"date-time":"2024-05-29T03:18:42Z","timestamp":1716952722000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":4,"title":["Synthesis and in vitro cytotoxicity of benzoxazole\u2010based PPAR\u03b1\/\u03b3 antagonists in colorectal cancer cell lines"],"prefix":"10.1002","volume":"357","author":[{"given":"Nazaret","family":"Moreno\u2010Rodr\u00edguez","sequence":"first","affiliation":[{"name":"Departamento de Qu\u00edmica Org\u00e1nica y Farmac\u00e9utica, Facultad de Farmacia Universidad de Sevilla Sevilla Spain"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Antonio","family":"Laghezza","sequence":"additional","affiliation":[{"name":"Department of Pharmacy\u2010Drug 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