Design, synthesis and biological activity evaluation of novel anticancer agent 5-(2-carboxyethenyl)indole derivatives

A series of novel 5-(2-Carboxyethenyl) indole derivatives were designed and synthesized about 38-48% overall yields. Two of the seven newly synthesized compounds, compound 5 and 7, have not been reported before. Their structures were characterized on the basis of H, C NMR, and those compounds were tested for their anticancer activities against K562 and HT-29 cell lines. Results indicated that compounds 5, 6 and 7 containing 5-(2-Carboxyethenyl)indole derivatives demonstrated significant anticancer activity against HT-29 cell, their potency reached 4.67, 8.24 and 6.73 μM, respectively.