{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,25]],"date-time":"2025-10-25T12:24:03Z","timestamp":1761395043801,"version":"build-2065373602"},"reference-count":20,"publisher":"Wiley","issue":"15","license":[{"start":{"date-parts":[[2017,7,19]],"date-time":"2017-07-19T00:00:00Z","timestamp":1500422400000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["chemistry-europe.onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["ChemMedChem"],"published-print":{"date-parts":[[2017,8,8]]},"abstract":"<jats:title>Abstract<\/jats:title><jats:p>STAT5 is a transcription factor, a member of the STAT family of signaling proteins. STAT5 is involved in many types of cancer, including chronic myelogenous leukemia (CML), in which this protein is found constitutively activated as a consequence of BCR\u2010ABL expression. The neuroleptic drug pimozide was recently reported to act as an inhibitor of STAT5 phosphorylation and is capable of inducing apoptosis in CML cells in\u2005vitro. Our research group has synthesized simple derivatives of pimozide with cytotoxic activity and that are able to decrease the levels of phosphorylated STAT5. In this work we continued the search for novel STAT5 inhibitors, synthesizing compounds in which the benzoimidazolinone ring of pimozide is either maintained or modified, in order to obtain further structure\u2013activity relationship information for this class of STAT5 inhibitors. Two compounds of the series showed potent cytotoxic activity against BCR\u2010ABL\u2010positive and pSTAT5\u2010overexpressing K562 cells and were able to markedly decrease the levels of phosphorylated STAT5.<\/jats:p>","DOI":"10.1002\/cmdc.201700234","type":"journal-article","created":{"date-parts":[[2017,6,28]],"date-time":"2017-06-28T11:08:54Z","timestamp":1498648134000},"page":"1183-1190","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":21,"title":["Effects of Pimozide Derivatives on pSTAT5 in K562 Cells"],"prefix":"10.1002","volume":"12","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-9135-6624","authenticated-orcid":false,"given":"Riccardo","family":"Rondanin","sequence":"first","affiliation":[{"name":"Dipartimento di Scienze Chimiche e Farmaceutiche Universit\u00e0 di Ferrara  via Fossato di Mortara 17 44121 Ferrara Italy"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-1701-9045","authenticated-orcid":false,"given":"Daniele","family":"Simoni","sequence":"additional","affiliation":[{"name":"Dipartimento di Scienze Chimiche e Farmaceutiche Universit\u00e0 di Ferrara  via Fossato di Mortara 17 44121 Ferrara Italy"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Martina","family":"Maccesi","sequence":"additional","affiliation":[{"name":"Dipartimento di Scienze Chimiche e Farmaceutiche Universit\u00e0 di Ferrara  via Fossato di Mortara 17 44121 Ferrara Italy"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6374-773X","authenticated-orcid":false,"given":"Romeo","family":"Romagnoli","sequence":"additional","affiliation":[{"name":"Dipartimento di Scienze Chimiche e Farmaceutiche Universit\u00e0 di Ferrara  via Fossato di Mortara 17 44121 Ferrara Italy"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Stefania","family":"Grimaudo","sequence":"additional","affiliation":[{"name":"Dipartimento Biomedico di Medicina Interna e Specialistica Universit\u00e0 di Palermo  via del Vespro 129 90127 Palermo Italy"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Rosaria Maria","family":"Pipitone","sequence":"additional","affiliation":[{"name":"Dipartimento Biomedico di Medicina Interna e Specialistica Universit\u00e0 di Palermo  via del Vespro 129 90127 Palermo Italy"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Maria","family":"Meli","sequence":"additional","affiliation":[{"name":"Dipartimento di Scienze per la Promozione della Salute e Materno Infantile Universit\u00e0 di Palermo  via del Vespro 129 90127 Palermo Italy"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Antonio","family":"Cascio","sequence":"additional","affiliation":[{"name":"Dipartimento di Scienze per la Promozione della Salute e Materno Infantile Universit\u00e0 di Palermo  via del Vespro 129 90127 Palermo Italy"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Manlio","family":"Tolomeo","sequence":"additional","affiliation":[{"name":"Dipartimento di Scienze per la Promozione della Salute e Materno Infantile, Centro Interdipartimentale di Ricerca in Oncologia Clinica Universit\u00e0 di Palermo  via del Vespro 129 902127 Palermo Italy"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2017,7,19]]},"reference":[{"key":"e_1_2_7_1_1","doi-asserted-by":"crossref","first-page":"651","DOI":"10.1038\/nrm909","volume":"3","author":"Levy D. 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