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

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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

Anti-Cancer Agents in Medicinal Chemistry, 15(8): 955-969.

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

Affiliation: Department of Pharmaceutical Chemistry, H. R. Patel Institute of Pharmaceutical Education and Research, Shirpur, District, Dhule -425405, Maharashtra, India.


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.


Anticancer, antineoplastic, combretastatin, combretastatin analogues, cytotoxicity, natural products, SAR, tubulin inhibitors, vascular disrupting agent.

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Article Details

Volume: 15
Issue Number: 8
First Page: 955
Last Page: 969
Page Count: 15
DOI: 10.2174/1871520615666150526141259
Price: $58

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