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Combination therapies play a pivotal role in cancer treatment due to the intricate nature of the disease. Tubulin, a protein crucial for cellular functions, is a prime target in tumor therapy as it regulates microtubule dynamics. Combining tubulin inhibitors with other different inhibitors as dual targeting inhibitors has shown synergistic anti-tumor effects, amplifying therapeutic outcomes. Despite clinical approval of several tubulin inhibitors, their efficacy is hampered by drug resistance and toxic side effects. Dual targeting inhibitors of tubulin and other cancer-related pathways have emerged as vital components in cancer therapy, with promising prospects in both market availability and ongoing clinical trials. The rational design of hybrid inhibitors targeting both pathways presents an innovative approach to combatting cancer. However, despite the potent anti-tumor activity exhibited by several compounds, research on their anti-angiogenic potential remains limited. This review emphasizes the significance of tubulin based dual-target inhibitors, elucidating their mechanisms of action. Recent advances in exploring therapeutic efficacy, toxicity profiles, and challenges such as MDR are discussed. By presenting the research progress of tubulin based dual-target inhibitors as potential anticancer agents, this study delivers valuable insights for the development of more efficient drugs for cancer therapy. Copyright © 2025 Elsevier Inc. All rights reserved.

Citation

Prasanna Anjaneyulu Yakkala, Ahmed Kamal. Dual-targeting inhibitors involving tubulin for the treatment of cancer. Bioorganic chemistry. 2025 Mar;156:108116

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PMID: 39823818

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