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The chosen group was further evaluated for antiproliferative effects on 1321N1 astrocytoma cells, along with U87MG, U-251, and LN-229 glioblastoma cell lines. Certain compounds were subjected to in vitro absorption, distribution, metabolism, excretion, and toxicity (ADMET) testing, for assessing factors such as lipophilicity, plasma protein binding, phospholipid affinity, potential for drug\u2013drug interactions (DDI), membrane permeability (PAMPA), metabolic stability, and hepatotoxicity. Additionally, in vivo testing was performed using the Danio rerio model. The developed group includes the selective 5-HT6R antagonist PP 15, dual ligand for 5-HT1AR\/5-HT6R PP 13, and dual ligand for 5-HT5AR\/5-HT6R PP 10. The use of multifunctional ligands was associated with high anticancer activity both against selected glioma cell lines and other cancers (IC50 &amp;lt; 25 \u03bcM).<\/jats:p>","DOI":"10.1021\/acsomega.4c06456","type":"journal-article","created":{"date-parts":[[2025,2,11]],"date-time":"2025-02-11T15:05:27Z","timestamp":1739286327000},"page":"6446-6469","source":"Crossref","is-referenced-by-count":2,"title":["Long-Chain Cyclic\nArylguanidines as Multifunctional\nSerotonin Receptor Ligands with Antiproliferative Activity"],"prefix":"10.1021","volume":"10","author":[{"ORCID":"https:\/\/orcid.org\/0000-0003-4880-8044","authenticated-orcid":true,"given":"Przemys\u0142aw","family":"Zare\u0328ba","sequence":"first","affiliation":[{"name":"Cracow University of Technology , , 24 Warszawska Street , ,","place":["Cracow, Poland, 31-155"]}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Anna K.","family":"Drabczyk","sequence":"additional","affiliation":[{"name":"Cracow University of 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