2-Phenylindole derivatives as anticancer agents: synthesis and screening against murine melanoma, human lung and breast cancer cell lines

Abstract

Indole derivatives have attractive anticancer properties and may be a future hope for better anticancer drug(s) of low toxicity and high potency. In this paper, syntheses of 2-phenylindole derivatives have been described via Fischer indole synthesis through a one-pot solvent-free method. The synthesized compounds were screened for anticancer potential in vitro against murine melanoma (B16F10), human lung cancer (A549), and human breast cancer (MDA-MB-231) cell lines. The results highlighted that 2-phenylindole derivatives are also promising anticancer agents in case of melanoma and lung cancer along with the breast cancer. Molecular docking analyses with possible targets for melanoma (NEDD4-1) and lung cancer (EGFR) were also performed to understand specific interactions of 2-phenylindole derivatives with the amino acid residues of the receptors.

GRAPHICAL ABSTRACT

KEYWORDS:

• A549
• B16F10
• anticancer activity
• Fischer indole synthesis
• MDA-MB-231
• molecular docking
• 2-phenylindole

Acknowledgments

The authors thank Sophisticated Instrumentation Center, Dr. Harisingh Gour University, Sagar, for recording NMR spectral data and HRMS of our compounds.

Additional information

Funding

SG and KD are thankful to the University Grants Commission (UGC), New Delhi for Startup grants No. F.30-106/2015-BSR and No. F.30-56/2014 BSR, respectively.