Antimitotic activities of 2-phenylindole-3-carbaldehydes in human breast cancer cells

Small molecules such as indoles are attractive as inhibitors of tubulin polymerization. Thus a number of 2-phenylindole-3-carbaldehydes with lipophilic substituents in both aromatic rings was synthesized and evaluated for antitumor activity in MDA-MB 231 and MCF-7 breast cancer cells. Some 5-alkylindole derivatives with a 4-methoxy group in the 2-phenyl ring strongly inhibit the growth of breast cancer cells with IC50 values of 5–20 nM. Their action can be rationalized by the cell cycle arrest in G2/M phase due to the inhibition of tubulin polymerization.

5-n-Alkyl-2-phenylindole-3-carbaldehydes strongly inhibit the growth of MDA-MB 231 breast cancer cells (IC50: 5–20 nM) through interference with tubulin polymerization and subsequent cell cycle arrest in G2/M phase.Figure optionsDownload as PowerPoint slide