{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,18]],"date-time":"2026-08-18T18:24:15Z","timestamp":1787077455533,"version":"build-2736575974"},"reference-count":41,"publisher":"American Chemical Society (ACS)","issue":"25","license":[{"start":{"date-parts":[[2025,6,18]],"date-time":"2025-06-18T00:00:00Z","timestamp":1750204800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/100016906","name":"Fundacja Uniwersytetu im. Adama Mickiewicza","doi-asserted-by":"publisher","award":["NA"],"award-info":[{"award-number":["NA"]}],"id":[{"id":"10.13039\/100016906","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100004569","name":"Ministerstwo Edukacji i Nauki","doi-asserted-by":"publisher","award":["0159\/DIA\/2020\/49"],"award-info":[{"award-number":["0159\/DIA\/2020\/49"]}],"id":[{"id":"10.13039\/501100004569","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2025,7,1]]},"abstract":"<jats:title>Abstract<\/jats:title>\n                  <jats:p>Ivermectin (IVR), whose discovery has been Nobel-Prize-honored, is a 16-membered macrocyclic lactone used in medicine as an extremely effective and safe antiparasitic drug. In recent years, interest in this compound has grown due to its potential effectiveness in killing various types of cancer cells. However, research on the anticancer activity of IVR derivatives is limited. Additionally, the growing problem of drug resistance raises concerns about the effectiveness of this drug in the treatment of parasitic diseases. Therefore, in this work, we provide a detailed description of the synthesis of ten new IVR bioconjugates with compounds exhibiting high anticancer and\/or antimicrobial activity. We also assess the effectiveness of these hybrids in killing Trypanosoma brucei brucei a protozoan parasite that causes African trypanosomiasis, as well as their anticancer activity toward various cancer cell lines. Many of the newly synthesized conjugates exhibited higher biological activity than their respective parent compounds as well as increased selectivity indices. The IVR conjugate with artesunate (compound 16) appears particularly interesting, as it proved not only to be several times more active than the parent compounds but also showed no toxicity toward a reference cell line, indicating its potential as a therapeutic agent.<\/jats:p>","DOI":"10.1021\/acsomega.5c02998","type":"journal-article","created":{"date-parts":[[2025,6,18]],"date-time":"2025-06-18T08:17:15Z","timestamp":1750234635000},"page":"27380-27392","source":"Crossref","is-referenced-by-count":2,"title":["Antiproliferative\nand Trypanocidal Activity of Ivermectin\nBioconjugates"],"prefix":"10.1021","volume":"10","author":[{"given":"Micha\u0142","family":"Sulik","sequence":"first","affiliation":[{"name":"Adam Mickiewicz University , , Uniwersytetu Poznan\u0301skiego 8 , ,","place":["Poznan\u0301, Poland, 61\u2212614"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dagmara","family":"Otto-S\u0301lusarczyk","sequence":"additional","affiliation":[{"name":"Medical University of Warsaw , , Banacha 1 , ,","place":["Warsaw, Poland, 02\u2212097"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Dietmar","family":"Steverding","sequence":"additional","affiliation":[{"name":"University of East Anglia , , ,","place":["Norwich, U.K., NR4 7TJ"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Marta","family":"Struga","sequence":"additional","affiliation":[{"name":"Medical University of Warsaw , , Banacha 1 , ,","place":["Warsaw, Poland, 02\u2212097"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-4770-215X","authenticated-orcid":true,"given":"Adam","family":"Huczyn\u0301ski","sequence":"additional","affiliation":[{"name":"Adam Mickiewicz University , , Uniwersytetu Poznan\u0301skiego 8 , ,","place":["Poznan\u0301, Poland, 61\u2212614"]}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"316","published-online":{"date-parts":[[2025,6,18]]},"reference":[{"key":"2026081811283275700_cit1","unstructured":"World Health Organization\n          . Cancer, https:\/\/www.who.int\/news-room\/fact-sheets\/detail\/cancer. (on-line access: 2025\u201304\u201302)"},{"key":"2026081811283275700_cit2","unstructured":"Global Cancer Observatory\n          , https:\/\/gco.iarc.fr\/. 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Drug Delivery Rev."},{"issue":"5","key":"2026081811283275700_cit6","doi-asserted-by":"publisher","first-page":"495","DOI":"10.1038\/ja.2017.11","article-title":"Ivermectin:\nenigmatic multifaceted \u2019wonder\u2019 drug continues to surprise\nand exceed expectations","volume":"70","author":"Crump","year":"2017","journal-title":"J. Antibiot (Tokyo)"},{"issue":"6","key":"2026081811283275700_cit7","doi-asserted-by":"publisher","first-page":"853","DOI":"10.2174\/138920112800399095","article-title":"History\nof Avermectin and Ivermectin, with Notes on the History of Other Macrocyclic\nLactone Antiparasitic Agents","volume":"13","author":"Campbell","year":"2012","journal-title":"Curr. Pharm. Biotechnol."},{"key":"2026081811283275700_cit8","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2023.115838","article-title":"Antiparasitic\nActivity of Ivermectin: Four Decades of Research into a \u201cWonder\nDrug.\u201d","volume":"261","author":"Sulik","year":"2023","journal-title":"Eur. J. 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Chem."},{"issue":"6","key":"2026081811283275700_cit34","doi-asserted-by":"publisher","first-page":"569","DOI":"10.1016\/j.trechm.2020.03.007","article-title":"Recent Fascinating\nAspects of the CuAAC Click Reaction","volume":"2","author":"Meldal","year":"2020","journal-title":"Trends\nChem."},{"key":"2026081811283275700_cit35","doi-asserted-by":"publisher","first-page":"510","DOI":"10.1016\/j.ejmech.2018.07.021","article-title":"Biological Activity\nof Doubly Modified Salinomycin\nAnalogs\u2013Evaluation in Vitro and Ex Vivo","volume":"156","author":"Antoszczak","year":"2018","journal-title":"Eur. J. Med. Chem."},{"key":"2026081811283275700_cit36","doi-asserted-by":"publisher","DOI":"10.1016\/j.ejmech.2022.114777","article-title":"Triterpenoid Pyrazines and Pyridines\u2013Synthesis, Cytotoxicity,\nMechanism of Action, Preparation of Prodrugs","volume":"243","author":"Hodon\u030c","year":"2022","journal-title":"Eur. J. Med. 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Gambiense","volume":"4","author":"Baltz","year":"1985","journal-title":"EMBO J."},{"issue":"4","key":"2026081811283275700_cit41","doi-asserted-by":"publisher","first-page":"257","DOI":"10.1016\/0001-706X(93)90083-N","article-title":"A Comparison of\nThree Methods of Estimating EC50 in Studies of Drug Resistance\nof Malaria Parasites","volume":"55","author":"Huber","year":"1993","journal-title":"Acta Trop."}],"container-title":["ACS Omega"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/pubs.acs.org\/doi\/pdf\/10.1021\/acsomega.5c02998","content-type":"application\/pdf","content-version":"vor","intended-application":"unspecified"},{"URL":"https:\/\/pubs.acs.org\/acsodf\/article-pdf\/10\/25\/27380\/40840181\/ao5c02998.pdf","content-type":"application\/pdf","content-version":"vor","intended-application":"syndication"},{"URL":"https:\/\/pubs.acs.org\/acsodf\/article-pdf\/10\/25\/27380\/40840181\/ao5c02998.pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2026,8,18]],"date-time":"2026-08-18T17:24:47Z","timestamp":1787073887000},"score":1,"resource":{"primary":{"URL":"https:\/\/pubs.acs.org\/acsodf\/article\/10\/25\/27380\/3654844\/Antiproliferative-and-Trypanocidal-Activity-of"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2025,6,18]]},"references-count":41,"journal-issue":{"issue":"25","published-online":{"date-parts":[[2025,6,18]]},"published-print":{"date-parts":[[2025,7,1]]}},"URL":"https:\/\/doi.org\/10.1021\/acsomega.5c02998","relation":{},"ISSN":["2470-1343"],"issn-type":[{"value":"2470-1343","type":"electronic"}],"subject":[],"published":{"date-parts":[[2025,6,18]]}}}