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2-Phenylindole derivatives as anticancer agents: synthesis and screening against murine melanoma,human lung and breast cancer cell lines
Authors:Ruchi Gaikwad  Yamini Bobde  Routholla Ganesh  Tarun Patel  Anju Rathore  Balaram Ghosh
Affiliation:1. Laboratory of Drug Design and Discovery, Department of Pharmaceutical Sciences, Dr. H. S. Gour University, Sagar, India;2. Department of Pharmacy, BITS-Pilani, Hyderabad Campus, Hyderabad, India
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.
Keywords:A549  B16F10  anticancer activity  Fischer indole synthesis  MDA-MB-231  molecular docking  2-phenylindole
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