The natural stilbenoids combretastatin A-4 (CA4) and combretastatin A-1 (CA1) are potent antitubulin
agents demonstrating antimitotic activity as well as tumor vascular disruption property. Due to structural
simplicity and potent cytotoxicity of CA4 and CA1, they are considered as promising leads for the development of
potent anticancer agents. In fact, scientific fraternity is motivated to synthesize several derivatives of CA4 and
CA1 as novel therapeutic agents. In the literature, several studies have been carried out to evaluate the medicinal
chemistry, pharmacology and structure–activity relationships (SAR) of a variety of modified combretastatin derivatives. The present
report aimed at comprehensively revising the recent advancements (2006-2014) in the medicinal chemistry and SAR of diversified
combretastatin analogues. The published data concerning new combretastatin A-4 analogues as antimitotic anticancer agents are
presented and SAR is reviewed and discussed.
Keywords: Anticancer, antineoplastic, combretastatin, combretastatin analogues, cytotoxicity, natural products, SAR, tubulin inhibitors,
vascular disrupting agent.
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