Synthesis and bio-evaluation of quaternary centered 3-hydroxy-3-(trifluoromethyl)indolin-2-one derivatives for anticancer and antimicrobial activities
| Autor: | Raktani Bikshapathi, R. Maheshwari, G. Jagadeeshkumar, Rajesh Pamanji, U. S. N. Murty, V. Jayathirtha Rao, B. Yashwanth, J. Venkateswara Rao, Parvathaneni Sai Prathima |
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| Rok vydání: | 2016 |
| Předmět: |
Trifluoromethyl
biology 010405 organic chemistry Stereochemistry In silico Cyclin-dependent kinase 2 Protein Data Bank (RCSB PDB) Biological activity General Chemistry 010402 general chemistry Antimicrobial 01 natural sciences In vitro 0104 chemical sciences chemistry.chemical_compound chemistry biology.protein Antibacterial activity |
| Zdroj: | Monatshefte für Chemie - Chemical Monthly. 148:757-764 |
| ISSN: | 1434-4475 0026-9247 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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