{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,2]],"date-time":"2026-09-02T23:13:35Z","timestamp":1788390815301,"version":"build-2803163510"},"reference-count":33,"publisher":"American Chemical Society (ACS)","issue":"18","license":[{"start":{"date-parts":[[2014,9,25]],"date-time":"2014-09-25T00:00:00Z","timestamp":1411603200000},"content-version":"vor","delay-in-days":17,"URL":"https:\/\/pubs.acs.org\/page\/policy\/authorchoice_ccby_termsofuse.html"}],"funder":[{"DOI":"10.13039\/100004440","name":"Wellcome Trust","doi-asserted-by":"publisher","award":["077705"],"award-info":[{"award-number":["077705"]}],"id":[{"id":"10.13039\/100004440","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100004440","name":"Wellcome Trust","doi-asserted-by":"publisher","award":["WT083481"],"award-info":[{"award-number":["WT083481"]}],"id":[{"id":"10.13039\/100004440","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2014,9,25]]},"abstract":"<jats:title>Abstract<\/jats:title>\n                  <jats:p>Glycogen synthase kinase 3 (GSK3) is a genetically validated drug target for human African trypanosomiasis (HAT), also called African sleeping sickness. We report the synthesis and biological evaluation of aminopyrazole derivatives as Trypanosoma brucei GSK3 short inhibitors. Low nanomolar inhibitors, which had high selectivity over the off-target human CDK2 and good selectivity over human GSK3\u03b2 enzyme, have been prepared. These potent kinase inhibitors demonstrated low micromolar levels of inhibition of the Trypanosoma brucei brucei parasite grown in culture.<\/jats:p>","DOI":"10.1021\/jm500239b","type":"journal-article","created":{"date-parts":[[2014,9,8]],"date-time":"2014-09-08T12:54:08Z","timestamp":1410180848000},"page":"7536-7549","source":"Crossref","is-referenced-by-count":27,"title":["The Design and Synthesis of\nPotent and Selective Inhibitors\nof\n                    <i>Trypanosoma brucei<\/i>\n                    Glycogen Synthase\nKinase 3 for the Treatment of Human African Trypanosomiasis"],"prefix":"10.1021","volume":"57","author":[{"given":"Robert","family":"Urich","sequence":"first","affiliation":[{"name":"University of Dundee , , Sir James Black Centre, Dow Street , ,","place":["Dundee, U.K., DD1 5EH"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Raffaella","family":"Grimaldi","sequence":"additional","affiliation":[{"name":"University of Dundee , , Sir James Black Centre, Dow Street , ,","place":["Dundee, U.K., DD1 5EH"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Torsten","family":"Luksch","sequence":"additional","affiliation":[{"name":"University of Dundee , , Sir James Black Centre, Dow Street , ,","place":["Dundee, U.K., DD1 5EH"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Julie A.","family":"Frearson","sequence":"additional","affiliation":[{"name":"University of Dundee , , Sir James Black Centre, Dow Street , ,","place":["Dundee, U.K., DD1 5EH"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ruth","family":"Brenk","sequence":"additional","affiliation":[{"name":"University of Dundee , , Sir James Black Centre , ,","place":["Dundee, U.K., DD1 5EH"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Paul G.","family":"Wyatt","sequence":"additional","affiliation":[{"name":"University of Dundee , , Sir James Black Centre, Dow Street , ,","place":["Dundee, U.K., DD1 5EH"]}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"316","published-online":{"date-parts":[[2014,9,8]]},"reference":[{"key":"2026090218165727200_cit1","doi-asserted-by":"crossref","first-page":"727","DOI":"10.1038\/nrd1824","article-title":"Opportunities and challenges\nin antiparasitic drug discovery","volume":"4","author":"Pink","year":"2005","journal-title":"Nature Rev.\nDrug Discovery"},{"key":"2026090218165727200_cit2","doi-asserted-by":"crossref","first-page":"321","DOI":"10.1002\/cmdc.201000442","article-title":"Synthesis and Evaluation\nof Indatraline-Based Inhibitors\nfor Trypanothione Reductase","volume":"6","author":"Walton","year":"2011","journal-title":"ChemMedChem"},{"key":"2026090218165727200_cit3","doi-asserted-by":"crossref","first-page":"488","DOI":"10.1016\/j.pt.2003.09.002","article-title":"Chemotherapy\nof human African trypanosomiasis: current and future prospects","volume":"19","author":"Fairlamb","year":"2003","journal-title":"Trends Parasitol."},{"key":"2026090218165727200_cit4","doi-asserted-by":"crossref","first-page":"232","DOI":"10.1038\/nature10771","article-title":"High-throughput decoding of antitrypanosomal drug efficacy and resistance","volume":"482","author":"Alsford","year":"2012","journal-title":"Nature"},{"key":"2026090218165727200_cit5","doi-asserted-by":"crossref","first-page":"1249","DOI":"10.1016\/j.ijpara.2006.06.013","article-title":"Inhibitors of casein\nkinase 1 block the growth of Leishmania major promastigotes in vitro","volume":"36","author":"Allocco","year":"2006","journal-title":"Int. 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