Ethyl 6-amino-2-substituent-indole-3-carboxylate was synthesized via S_NAr reaction, reduction and tandem cyclization from 2,4-dinitrochlorobenzene and ethyl acetoacetate. The reaction of ethyl 6-amino-2-methylindole-3-carboxylate with ethyl acetoacetate in the presence of catalyst gave an enamine compound, and then ethyl 9-hydroxy-2,7-dimethylpyrrolo(2,3-f)quinoline-3-carboxylate was obtained by cyclization. Similarly, ethyl 6-amino-2-phenylindole-3-carboxylate and ethyl 6-amino-2-fur-2'-ylindole-3- carboxylate were synthesized. The structures of compounds were determined by ¹H NMR, IR and MS spectra. These compounds were assayed with inhibitory activity against lung cancer A549 cell growth, and the inhibitory effect on the cell viability was dose-dependent.

Key words: reduction, growth inhibitory activity, cyclization, lung cancer cell A549, indole derivative