Combretastatin A-4 and its analogs in cancer therapy

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Combretastatin A-4 (CA-4) is an anti-mitotic agent that is gaining rapid recognition among cancer biologists and clinicians as one of the newer vascular disrupting agents, (VDAs) for cancer therapy. CA-4 belongs to a group of tubulin binding natural products called combretastatin, derived from the African Bush Willow, Combretum caffrum. Due to CA-4′s in vivo efficacy, a number of analogs of CA-4 have been synthesized to maximize its solubility and bioavailability. Combretastatin A-4 phosphate is a more soluble form of CA-4 that has successfully completed phase I trial and is currently under phase II/III trials for treatment of acute myelogenous leukemia and relapsed ovarian cancer. This review attempts to highlight the various CA-4 analogs that have been synthesized and their effectiveness in clinical trials as VDAs.

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International Journal of Pharmaceutical Sciences Review and Research

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