Miscellaneous Anticancer Drugs Acting On Novel Sites On Tubuline

Estramustine phosphate, mentioned in Section 2.4, is used in the treatment of advanced metastatic prostate cancer, alone or in combination with other antitu-bulin agents such as vinblastine, paclitaxel, or ixabepilone.70 It is administered as a phosphate prodrug, which is inactive because it does not enter the cells but is rapidly metabolized to the active species. Estramustine depolymerizes microtubule networks, inhibiting cell growth and inducing mitotic arrest, by binding to a site different from other drugs.71

NSC-639829 is a representative of the benzoylphenylurea (BPU) class of com-pounds,72 which were developed initially as insecticides but showed antitumor activity in random screening. It inhibits tubulin polymerization by binding to a novel site and is being evaluated in clinical trials in patients with refractory metastatic cancer.73 NSC-639829 is also a potent inhibitor of DNA polymerase.

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