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Structural variations (chlorine, bromine, iodine, and cyano groups) were introduced at position\u20057 of 4\u2010aza\u20107,9\u2010dideazaadenine. In addition, pyrrolo[2,1\u2010<jats:italic>f<\/jats:italic>][1,2,4]triazine <jats:italic>C<\/jats:italic>\u2010nucleosides bearing a 2\u2032\u2010deoxy\u2010, 2\u2032,3\u2032\u2010dideoxy\u2010, and 2\u2032,3\u2032\u2010dehydrodideoxyribose moiety were also prepared. Among these analogues, the pyrrolo[2,1\u2010<jats:italic>f<\/jats:italic>][1,2,4]triazine <jats:italic>C<\/jats:italic>\u2010ribonucleosides with either a hydrogen atom or cyano group at position\u20057 of the nucleobase displayed potent cytotoxic activity in a panel of various cancer cell lines.<\/jats:p>","DOI":"10.1002\/cmdc.201700657","type":"journal-article","created":{"date-parts":[[2017,11,21]],"date-time":"2017-11-21T10:22:36Z","timestamp":1511259756000},"page":"97-104","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":22,"title":["Synthesis and Biological Evaluation of Pyrrolo[2,1\u2010<i>f<\/i>][1,2,4]triazine <i>C<\/i>\u2010Nucleosides with a Ribose, 2\u2032\u2010Deoxyribose, and 2\u2032,3\u2032\u2010Dideoxyribose Sugar Moiety"],"prefix":"10.1002","volume":"13","author":[{"given":"Qingfeng","family":"Li","sequence":"first","affiliation":[{"name":"Medicinal Chemistry Rega Institute for Medical Research KU Leuven  Herestraat 49-bus 1041 3000 Leuven Belgium"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7066-4329","authenticated-orcid":false,"given":"Eveline","family":"Lescrinier","sequence":"additional","affiliation":[{"name":"Medicinal Chemistry Rega Institute for Medical Research KU Leuven  Herestraat 49-bus 1041 3000 Leuven Belgium"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Elisabetta","family":"Groaz","sequence":"additional","affiliation":[{"name":"Medicinal Chemistry Rega Institute for Medical Research KU Leuven  Herestraat 49-bus 1041 3000 Leuven Belgium"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Leentje","family":"Persoons","sequence":"additional","affiliation":[{"name":"Laboratory of Virology and Chemotherapy Rega Institute for Medical Research KU Leuven  Herestraat 49-bus 1043 3000 Leuven Belgium"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7092-1153","authenticated-orcid":false,"given":"Dirk","family":"Daelemans","sequence":"additional","affiliation":[{"name":"Laboratory of Virology and Chemotherapy Rega Institute for Medical Research KU Leuven  Herestraat 49-bus 1043 3000 Leuven Belgium"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3589-8503","authenticated-orcid":false,"given":"Piet","family":"Herdewijn","sequence":"additional","affiliation":[{"name":"Medicinal Chemistry Rega Institute for Medical Research KU Leuven  Herestraat 49-bus 1041 3000 Leuven Belgium"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3872-6558","authenticated-orcid":false,"given":"Steven","family":"De\u2005Jonghe","sequence":"additional","affiliation":[{"name":"Laboratory of Virology and Chemotherapy Rega Institute for Medical Research KU Leuven  Herestraat 49-bus 1043 3000 Leuven Belgium"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"311","published-online":{"date-parts":[[2017,12,12]]},"reference":[{"key":"e_1_2_7_1_1","doi-asserted-by":"crossref","first-page":"447","DOI":"10.1038\/nrd4010","volume":"12","author":"Jordheim L. 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