Design, Synthesis and Biological Evaluation of Novel Aminosaccharide Derivatives of Combretastatin A-4

Author(s): Yan Tang, Zhewei Tu, Jing Sun, Xiong Zhu, Kun Liu, Shuying He, Yungen Xu

Journal Name: Letters in Drug Design & Discovery

Volume 10 , Issue 10 , 2013

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Combretastatin A-4 (CA-4), a natural vascular disrupting agent (VDA) with potent anti-cancer activity, is a promising lead compound in drug discovery. In view of the potential application of carbohydrates in medicinal chemistry, we designed and synthesized sixteen novel CA-4 aminosaccharide derivatives. In vitro anti-proliferative studies showed that compounds 7a and 7c significantly inhibited the growth of human umbilical vein endothelia cells (HUVEC) and other four cancer cell lines. Besides, preliminary structure-activity relationship (SAR) was summarized.

Keywords: Anti-cancer agent, Aminosaccharide, Combretastatin A-4 (CA-4), Vascular disrupting agent (VDA), Structural modification, Human umbilical vein endothelia cells (HUVEC).

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Article Details

Year: 2013
Published on: 24 October, 2013
Page: [935 - 941]
Pages: 7
DOI: 10.2174/15701808113109990024
Price: $65

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