Recent Advancement in Discovery and Development of Natural Product Combretastatin-inspired Anticancer Agents

Author(s): Pravin O. Patil, Ashwini G. Patil, Rajesh A. Rane, Pravin C. Patil, Prashant K. Deshmukh, Sanjay B. Bari, Dilip A. Patil, Shital S. Naphade

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 15 , Issue 8 , 2015

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Graphical Abstract:


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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Article Details

Year: 2015
Published on: 16 August, 2015
Page: [955 - 969]
Pages: 15
DOI: 10.2174/1871520615666150526141259
Price: $65

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