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This transport is the basis for an emerging approach to selective cancer cell destruction by using radioiodide after targeted NIS gene transfer. Therapeutic efficacy requires that radioiodide retention be maximized in tumor cells. A first generation of forty imidazo[2,1\u2010<\/jats:italic>b<jats:italic>]thiazole derivatives as iodide efflux inhibitors is described along with the evaluation of their biological properties. Structure\u2013activity relationship studies by using radioiodide uptake in rat thyroid\u2010derived cells (FRTL5) revealed that the 5,6\u2010dihydroimidazo[2,1\u2010<\/jats:italic>b<jats:italic>]thiazole heterocycle is required for activity. Introduction of electron\u2010donor substituents on the 3\u2010biphenyl moiety led to the discovery of novel potent compounds. A compound was identified with enhanced potency compared to reference <jats:bold>1<\/jats:bold>. These molecules give the possibility to increase the cellular retention of radioiodide in NIS\u2010expressing tumors, leading to higher absorbed doses and killing efficacy.<\/jats:italic><\/jats:p>","DOI":"10.1002\/cmdc.200900365","type":"journal-article","created":{"date-parts":[[2009,9,24]],"date-time":"2009-09-24T14:39:26Z","timestamp":1253803166000},"page":"1819-1830","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":3,"title":["Synthesis and Evaluation of Imidazo[2,1\u2010<i>b<\/i>]thiazoles as Iodide Efflux Inhibitors in Thyrocytes"],"prefix":"10.1002","volume":"4","author":[{"given":"Nathalie","family":"Lecat\u2010Guillet","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yves","family":"Ambroise","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2009,10,23]]},"reference":[{"key":"e_1_2_6_1_2","doi-asserted-by":"publisher","DOI":"10.1152\/physrev.2000.80.3.1083"},{"key":"e_1_2_6_2_2","first-page":"922","volume-title":"The Thyroid: a Fundamental and Clinical Text, 7th\u2005ed.","author":"Mazzaferri E. 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