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

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

Volume: 10 Issue: 10

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Tang Yan, Tu Zhewei, Sun Jing, Zhu Xiong, Liu Kun, He Shuying and Xu Yungen, Design, Synthesis and Biological Evaluation of Novel Aminosaccharide Derivatives of Combretastatin A-4, Letters in Drug Design & Discovery 2013; 10 (10) . https://dx.doi.org/10.2174/15701808113109990024