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Recently, we identified the partial PPAR\u03b3 agonist telmisartan as effective sensitizer of resistant K562 CML cells to imatinib treatment. Here, the importance of the heterocyclic core on the cell death\u2010modulating effects of the telmisartan\u2010derived lead 4\u2032\u2010((2\u2010propyl\u20101<jats:italic>H<\/jats:italic>\u2010benzo[<jats:italic>d<\/jats:italic>]imidazol\u20101\u2010yl)methyl)\u2010[1,1\u2032\u2010biphenyl]\u20102\u2010carboxylic acid (<jats:bold>3\u2009b<\/jats:bold>) was investigated. Inspired by the pharmacodynamics of HYL\u20106d and the selective PPAR\u03b3 ligand VSP\u201051, the benzimidazole was replaced by a carbazole or an indole core. The results indicate no correlation between PPAR\u03b3 activation and sensitization of resistant CML cells to imatinib. The 2\u2010COOH derivatives of the carbazoles or indoles achieved low activity at PPAR\u03b3, while the benzimidazoles showed 60\u2010100\u2009% activation. Among the 2\u2010CO<jats:sub>2<\/jats:sub>CH<jats:sub>3<\/jats:sub> derivatives, only the ester of the lead (<jats:bold>2\u2009b<\/jats:bold>) slightly activated PPAR\u03b3. Sensitizing effects were further observed for this non\u2010cytotoxic <jats:bold>2\u2009b<\/jats:bold> (80\u2009% cell death), and to a lesser extent for the lead <jats:bold>3\u2009b<\/jats:bold> or the 5\u2010Br\u2010substituted ester of the benzimidazoles (<jats:bold>5\u2009b<\/jats:bold>).<\/jats:p>","DOI":"10.1002\/cmdc.202000092","type":"journal-article","created":{"date-parts":[[2020,4,16]],"date-time":"2020-04-16T13:01:00Z","timestamp":1587042060000},"page":"1067-1077","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":6,"title":["Synthesis and Characterization of Telmisartan\u2010Derived Cell Death Modulators to Circumvent Imatinib Resistance in Chronic Myeloid Leukemia"],"prefix":"10.1002","volume":"15","author":[{"given":"Anna M.","family":"Schoepf","sequence":"first","affiliation":[{"name":"Department of Pharmaceutical Chemistry Institute of Pharmacy CMBI \u2013 Center for Molecular Biosciences Innsbruck University of Innsbruck, CCB \u2013 Centrum for Chemistry and Biomedicine  Innrain 80\/82 6020 Innsbruck Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Stefan","family":"Salcher","sequence":"additional","affiliation":[{"name":"Tyrolean Cancer Research Institute  Innrain 66 6020 Innsbruck Austria"},{"name":"Department of Internal Medicine V Medical University Innsbruck  Anichstra\u00dfe 35 6020 Innsbruck Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Verena","family":"Hohn","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry Institute of Pharmacy CMBI \u2013 Center for Molecular Biosciences Innsbruck University of Innsbruck, CCB \u2013 Centrum for Chemistry and Biomedicine  Innrain 80\/82 6020 Innsbruck Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Florina","family":"Veider","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry Institute of Pharmacy CMBI \u2013 Center for Molecular Biosciences Innsbruck University of Innsbruck, CCB \u2013 Centrum for Chemistry and Biomedicine  Innrain 80\/82 6020 Innsbruck Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Petra","family":"Obexer","sequence":"additional","affiliation":[{"name":"Tyrolean Cancer Research Institute  Innrain 66 6020 Innsbruck Austria"},{"name":"Department of Pediatrics II Medical University Innsbruck  Innrain 66 6020 Innsbruck Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-0427-4012","authenticated-orcid":false,"given":"Ronald","family":"Gust","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry Institute of Pharmacy CMBI \u2013 Center for Molecular Biosciences Innsbruck University of Innsbruck, CCB \u2013 Centrum for Chemistry and Biomedicine  Innrain 80\/82 6020 Innsbruck Austria"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2020,5,6]]},"reference":[{"key":"e_1_2_8_1_1","doi-asserted-by":"publisher","DOI":"10.1182\/blood.V96.10.3343"},{"key":"e_1_2_8_2_1","doi-asserted-by":"publisher","DOI":"10.7326\/0003-4819-145-12-200612190-00008"},{"key":"e_1_2_8_3_1","doi-asserted-by":"publisher","DOI":"10.1517\/14712598.2014.867323"},{"key":"e_1_2_8_4_1","doi-asserted-by":"publisher","DOI":"10.1172\/JCI35721"},{"key":"e_1_2_8_5_1","doi-asserted-by":"publisher","DOI":"10.1172\/JCI85239"},{"key":"e_1_2_8_6_1","doi-asserted-by":"crossref","unstructured":"P. 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