1233979-32-2Relevant academic research and scientific papers
Synthesis and preliminary biological evaluation of novel taspine derivatives as anticancer agents
Zhang, Jie,Zhang, Yanmin,Shan, Yuanyuan,Li, Na,Ma, Wei,He, Langchong
, p. 2798 - 2805 (2010)
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 = 52.5 μM) and ECV304 (IC50 = 2.67 μM) 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.
