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:Department of Medicinal Chemistry China Pharmaceutical University Nanjing 210009 PR China.
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.
