Journal
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
Volume 16, Issue 8, Pages 942-960Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/1871520616666160204111832
Keywords
Combretastatin A-4; CA-4; Inhibitors of angiogenesis; Synthesis; Biological activity; Cancer therapy
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an ethylene bridge. CA-4, inhibitor of polymerization of tubulin to microtubules, possesses a strong antitumor and anti-vascular properties both in vitro and in vivo. Previous studies showed that disodium phosphate salt of CA-4, a water-soluble prodrug is well tolerated at therapeutically useful doses. However, it should be noted that the cis-configuration of the double bond and the 3,4,5-trimethoxy group on ring A is necessary for the biological activity of CA-4. Structure of CA-4 renders the compound readily susceptible to isomerization, which reduces the potency and bioavailability. To circumvent this problem, a lot of scientists in the world synthesized a series of cis-restricted CA-4 analogs, where the double bond has been replaced by introduction of non-heterocyclic groups or heterocyclic groups like beta-lactam and oxadiazole. This paper reviews the most important approaches in analogs of combretastatin synthesis and presents structure-reactivity relationships for these compounds.
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