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Chapter 14. Antimitotic Agents

1999; Elsevier BV; Linguagem: Inglês

10.1016/s0065-7743(08)60576-x

1557-8437

Qun Li, Hing L. Sham, Saul H. Rosenberg,

Cancer Treatment and Pharmacology

This chapter presents an overview of antimitotic agents. The clinical and commercial success of taxanes has stimulated a worldwide search for antimitotic agents that possess superior profiles. Antimitotic agents constitute a major class of cytotoxic drugs. Microtubules, which are the dynamic pipe-like protein fibers composed of alternating α- and β-tubulins, are integral components of the mitotic spindle which is intimately involved in cell replication. By interfering with the natural dynamics of tubulin polymerization or depolymerization, the antimitotic agents inhibit cell proliferation by arresting dividing cells in metaphase. Tubulin binding molecules have generated considerable interest among cytotoxic agents, due in part to the successful introduction of the taxanes into clinical oncology and to the widespread use of the vinca alkaloids. Renewed interest in antimitotic agents has been generated by the hope that non- multidrug-resistance (non-MDR) substrates that interact with tubulin at sites different from those of vinca alkaloids and taxanes can be discovered. The chapter presents concepts related to microtubule stabilizing compounds and describes vinca alkaloid site binders. An overview of colchicine-site binders (CCSB) is also presented.