First Report on 3-(3-oxoaryl) Indole Derivatives as Anticancer Agents: Microwave Assisted Synthesis, In Vitro Screening and Molecular Docking Studies

In this study ZrCl4 was identified as an efficient Lewis acid catalyst for the synthesis of 3-(3-oxoaryl) indole derivatives via microwave assisted Michael addition of 2-phenylindole with chalcones under solvent-free condition. The reaction proceeds smoothly with high efficiency under green reaction condition to afford a range of 3-(3-oxoaryl) indole derivatives exclusively within a short period of time in excellent yields. The synthesized compounds have shown promising in vitro anticancer activity against murine melanoma (B16F10) and human breast cancer (MCF7) cell lines. Molecular docking analysis showed that this type of indole derivatives may act as anticancer agents through the inhibition of tubulin polymerization.