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Synthesis and bio-evaluation of quaternary centered 3-hydroxy-3-(trifluoromethyl)indolin-2-one derivatives for anticancer and antimicrobial activities

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Abstract

A series of C(3)-trifluoromethylated compounds derived from N-substituted isatins were synthesized. The biological activity of all 3-hydroxy-3-(trifluoromethyl)indolin-2-one derivatives have been evaluated for in vitro cytotoxic activity and antibacterial activity. The active compounds were screened against nuclear xenobiotic receptor CAR (PDB ID: 1XLS), PIM1 kinase (PDB ID: 2O65), and CDK2 kinase (PDB ID: 3QHR) by using in silico molecular docking studies to obtain lead molecules. In addition to its potential anticancer activity, 5-bromo-3-ethynyl-3-hydroxy-1-(prop-2-yn-1-yl)indolin-2-one also showed specific antibacterial activity against S. aureus.

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Acknowledgments

P. S. P and V. J. R gratefully acknowledge to the financial assistance provided by the CSIR, Govt. of India, New Delhi 12th Five-year plan ORIGIN Project (CSC-0108). RBP (UGC-SRF), acknowledge for the fellowship provided by UGC, Govt of India.

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Correspondence to Parvathaneni Sai Prathima or V. Jayathirtha Rao.

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Bikshapathi, R., Prathima, P.S., Yashwanth, B. et al. Synthesis and bio-evaluation of quaternary centered 3-hydroxy-3-(trifluoromethyl)indolin-2-one derivatives for anticancer and antimicrobial activities. Monatsh Chem 148, 757–764 (2017). https://doi.org/10.1007/s00706-016-1764-0

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  • DOI: https://doi.org/10.1007/s00706-016-1764-0

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