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Recent Advances in Microtubule Targeting Agents for Cancer Therapy

Henrique C. Assunção, Patrícia M. A. Silva, Hassan Bousbaa, Honorina Cidade

2025Molecules18 citationsDOIOpen Access PDF

Abstract

Cancer mortality and the development of cancer resistance present significant challenges that must be addressed to ensure global health. 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-activity relationship (SAR) studies that could be important for the discovery of more effective MTAs in the future.

Topics & Concepts

Drug discoveryCancerCancer treatmentCancer drugsDrug resistanceCancer therapyDrugComputational biologyMedicinePharmacologyBiologyBioinformaticsMicrobiologyInternal medicineHistone Deacetylase Inhibitors ResearchClick Chemistry and ApplicationsSynthesis and biological activity
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