{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,18]],"date-time":"2026-09-18T05:03:08Z","timestamp":1789707788827,"version":"4.0.1"},"reference-count":41,"publisher":"MDPI AG","issue":"9","license":[{"start":{"date-parts":[[2026,9,11]],"date-time":"2026-09-11T00:00:00Z","timestamp":1789084800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Medical University of Silesia","award":["BNW-2-019\/N\/5\/E"],"award-info":[{"award-number":["BNW-2-019\/N\/5\/E"]}],"id":[{"id":"https:\/\/ror.org\/005k7hp45","id-type":"ROR","asserted-by":"crossref"}]},{"award":["BNW-2-019\/N\/5\/E"],"award-info":[{"award-number":["BNW-2-019\/N\/5\/E"]}],"id":[{"id":"https:\/\/ror.org\/005k7hp45","id-type":"ROR","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100011009","name":"Wroclawskie Centrum Sieciowo-Superkomputerowe","doi-asserted-by":"publisher","award":["431"],"award-info":[{"award-number":["431"]}],"id":[{"id":"10.13039\/501100011009","id-type":"DOI","asserted-by":"publisher"}]},{"award":["431"],"award-info":[{"award-number":["431"]}],"id":[{"id":"https:\/\/ror.org\/03fqwqm07","id-type":"ROR","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Biomolecules"],"abstract":"<jats:p>In recent years, extensive research has focused on fluoroquinolone\u2013triazole hybrids, with particular emphasis on structural modifications of ciprofloxacin. In the present study, novel derivatives of lomefloxacin with a 1,4-disubstituted-1,2,3-triazole moiety were designed, synthesised, and biologically evaluated at the N4 position of the piperazine ring. Molecular docking studies suggested potential interactions of the designed compounds with topoisomerase I, with docking scores comparable to that of the reference compound camptothecin. Molecular dynamics simulation suggested short-term conformational stability of the ligand-based (holo) topoisomerase II\u03b2 modulator. The synthesis was accomplished using a copper(I)-catalysed azide\u2013alkyne cycloaddition, leading to the formation of nine new compounds. A preliminary evaluation of antiproliferative activity was performed on selected human cancer cell lines using the WST-1 assay, while selectivity against normal human dermal fibroblast was assessed. The results obtained revealed promising antiproliferative activity of the tested derivatives, particularly against colorectal cancer cell lines.<\/jats:p>","DOI":"10.3390\/biom16091323","type":"journal-article","created":{"date-parts":[[2026,9,11]],"date-time":"2026-09-11T13:29:29Z","timestamp":1789133369000},"page":"1323","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Novel Lomefloxacin\u2013Triazole Hybrids: Design, Synthesis and In Vitro Antiproliferative Activity in Breast, Melanoma and Colon Cancer Cell Lines"],"prefix":"10.3390","volume":"16","author":[{"ORCID":"https:\/\/orcid.org\/0009-0007-8183-2974","authenticated-orcid":false,"given":"Justyna","family":"Nowakowska","sequence":"first","affiliation":[{"name":"Doctoral School, Medical University of Silesia, Poniatowskiego 15, 40-055 Katowice, Poland"},{"name":"Student Scientific Group, Department of Organic Chemistry, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia, Jagiello\u0144ska 4, 41-200 Sosnowiec, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-7892-0462","authenticated-orcid":false,"given":"Zuzanna","family":"Rzepka","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia, Jagiello\u0144ska 4, 41-200 Sosnowiec, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9842-1289","authenticated-orcid":false,"given":"Andrzej","family":"Bak","sequence":"additional","affiliation":[{"name":"Institute of Chemistry, University of Silesia, Szkolna 9, 40-007 Katowice, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6918-3330","authenticated-orcid":false,"given":"Dorota","family":"Wrze\u015bniok","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia, Jagiello\u0144ska 4, 41-200 Sosnowiec, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4631-2360","authenticated-orcid":false,"given":"Krzysztof","family":"Marciniec","sequence":"additional","affiliation":[{"name":"Department of Organic Chemistry, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia, Jagiello\u0144ska 4, 41-200 Sosnowiec, Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2026,9,11]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"18594","DOI":"10.1039\/D2RA02896D","article-title":"Recent Advances in Chemistry and Therapeutic Potential of Functionalized Quinoline Motifs\u2014A Review","volume":"12","author":"Ajani","year":"2022","journal-title":"RSC Adv."},{"key":"ref_2","doi-asserted-by":"crossref","first-page":"871","DOI":"10.1016\/j.ejmech.2014.07.044","article-title":"A Review on Anticancer Potential of Bioactive Heterocycle Quinoline","volume":"97","author":"Afzal","year":"2015","journal-title":"Eur. 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