Synthesis and preliminary biological evaluation of novel taspine derivatives as anticancer agents
- Eur J Med Chem. 2010 Jul;45(7):2798-805. doi: 10.1016/j.ejmech.2010.03.001.
- 1. School of Medicine, Xi'an Jiaotong University, Xi'an, 710061, P.R. China.
Antiangiogenic therapy might represent a new promising Anticancer therapeutic strategy. Taspine can significantly inhibit cell proliferation of human umbilical vein endothelial cells (HUVECs) induced by vascular endothelial growth factor-165, which is crucial for angiogenesis. In this study, a series of novel taspine derivatives were synthesized and screened for in vitro Anticancer and antiangiogenesis activities. The majority of the derivatives demonstrated a moderate degree of cytotoxicity against human Cancer cell lines. One of them (14) exhibited much better antiproliferative activity against CACO-2 (IC(50)=52.5microM) and ECV304 (IC(50)=2.67microM) cells than taspine did. Some of them were also effective in antiproliferative assays against HUVECs. The in silico estimate of solubility of title compounds were higher than that of taspine.