Fan Houxing
2009
Citations
0
Influential Citations
0
Citations
Quality indicators
Journal
Chinese Journal of Pharmaceuticals
Abstract
Started from 5-bromo-1H-indole,a series of new 3-substituted-5-fluoro-1,2-dihydro-3H-indol-2ones were synthesized via cyanation,Vilsmeier-Haack reaction,hydrolysis and condensation to give 3-(Z)-(5-FLuoro1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl-1H-indole-5-carboxylic acid,which was subjected to amination with the substituted amine.The in vitro antitumor activities of ten target compounds were evaluated against HMEC cell lines by MTT method with sunitinib as a positive control,and 1c,1f,1g and 1h showed better inhibitory activity against HMEC than sunitinib at the concentration of 10 μmol/L.Compounds 1c and 1e were selected to further evaluation on their anti-proliferation activities against SGC7901,A549,HL-60,SK-BR-3,HCT116 cell lines,the result showed that 1c and 1e had more potent anti-proliferation activities than sunitinib against HL-60 cell.