4.3 Article

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

Journal

SYNTHETIC COMMUNICATIONS
Volume 49, Issue 17, Pages 2258-2269

Publisher

TAYLOR & FRANCIS INC
DOI: 10.1080/00397911.2019.1620282

Keywords

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

Funding

  1. University Grants Commission (UGC), New Delhi [F.30-106/2015-BSR, F.30-56/2014 BSR]

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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.

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