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Among anticancer agents, microtubule-targeting agents (MTAs) represent a well-recognized therapeutic approach that disrupts microtubule dynamics, thereby inhibiting cell division, and has been widely used to treat several types of cancers. However, even though MTAs are widely regarded as effective, their potential is limited primarily due to cancer resistance and toxicity. Consequently, in the last years, the exploration of new MTAs with the aim of identifying agents with improved cytotoxicity, selectivity, and adequate pharmacokinetic profile, as well as the ability to evade drug resistance mechanisms, has remained a major concern in the development of anticancer treatment. This review highlights the discovery of new MTAs since 2020, with the goal of understanding the advancements made in this field and its future directions. Special attention is given to structure\u2013activity relationship (SAR) studies that could be important for the discovery of more effective MTAs in the future.<\/jats:p>","DOI":"10.3390\/molecules30163314","type":"journal-article","created":{"date-parts":[[2025,8,8]],"date-time":"2025-08-08T08:09:35Z","timestamp":1754640575000},"page":"3314","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":11,"title":["Recent Advances in Microtubule Targeting Agents for Cancer Therapy"],"prefix":"10.3390","volume":"30","author":[{"ORCID":"https:\/\/orcid.org\/0009-0008-7647-7477","authenticated-orcid":false,"given":"Henrique C.","family":"Assun\u00e7\u00e3o","sequence":"first","affiliation":[{"name":"Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Rua de Jorge de Viterbo Ferreira, 288, 4050-313 Porto, Portugal"},{"name":"CIIMAR\/CIMAR LA-Interdisciplinary Centre of Marine and Environmental Research, University of Porto, Terminal de Cruzeiros do Porto de Leix\u00f5es, 4450-208 Matosinhos, Portugal"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-0694-7321","authenticated-orcid":false,"given":"Patr\u00edcia M. A.","family":"Silva","sequence":"additional","affiliation":[{"name":"Associate Laboratory i4HB-Institute for Health and Bioeconomy, University Institute of Health Sciences-CESPU, 4585-116 Gandra, Portugal"},{"name":"UCIBIO-Applied Molecular Biosciences Unit, Translational Toxicology Research Laboratory, 1H-TOXRUN, IUCS-CESPU, University Institute of Health Sciences, 4585-116 Gandra, Portugal"},{"name":"UNIPRO\u2013Oral Pathology and Rehabilitation Research Unit, IUCS-CESPU, University Institute of Health Sciences, 4585-116 Gandra, Portugal"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-4006-5779","authenticated-orcid":false,"given":"Hassan","family":"Bousbaa","sequence":"additional","affiliation":[{"name":"UNIPRO\u2013Oral Pathology and Rehabilitation Research Unit, IUCS-CESPU, University Institute of Health Sciences, 4585-116 Gandra, Portugal"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0715-1779","authenticated-orcid":false,"given":"Honorina","family":"Cidade","sequence":"additional","affiliation":[{"name":"Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Rua de Jorge de Viterbo Ferreira, 288, 4050-313 Porto, Portugal"},{"name":"CIIMAR\/CIMAR LA-Interdisciplinary Centre of Marine and Environmental Research, University of Porto, Terminal de Cruzeiros do Porto de Leix\u00f5es, 4450-208 Matosinhos, Portugal"},{"name":"UNIPRO\u2013Oral Pathology and Rehabilitation Research Unit, IUCS-CESPU, University Institute of Health Sciences, 4585-116 Gandra, Portugal"}]}],"member":"1968","published-online":{"date-parts":[[2025,8,8]]},"reference":[{"key":"ref_1","first-page":"2794","article-title":"Suppression of centromere dynamics by Taxol in living osteosarcoma cells","volume":"63","author":"Kelling","year":"2023","journal-title":"Cancer Res."},{"key":"ref_2","first-page":"1101","article-title":"Pharmacological applications and in vitro biotechnological production of anticancer alkaloids of Catharanthus roseus","volume":"32","year":"2015","journal-title":"Biotecnol. 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