Synthesis and in vitro evaluation of 4-substituted furano[3,2-c] tetrahydroquinolines as potential anti-cancer agents
| Autor: | Can Chen, Qinglin Jiang, Dan Wang, Ting Wang, Mingyong Yuan, Sarah Zingales, Lulu Cai |
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| Rok vydání: | 2015 |
| Předmět: |
Stereochemistry
Antineoplastic Agents Apoptosis Inhibitory postsynaptic potential 01 natural sciences C6 cells 03 medical and health sciences Mice 0302 clinical medicine Cell Line Tumor Drug Discovery medicine Ic50 values Animals Furans Pharmacology Antitumor activity Molecular Structure 010405 organic chemistry Chemistry Cancer General Medicine medicine.disease In vitro 0104 chemical sciences Mitochondria Gene Expression Regulation Neoplastic 030220 oncology & carcinogenesis Quinolines Povarov reaction |
| Zdroj: | Journal of enzyme inhibition and medicinal chemistry. 31(5) |
| ISSN: | 1475-6374 |
| Popis: | A convenient and mild method for the synthesis of substituted furano [3,2-c]tetrahydroquinoline derivatives was developed, using the multi-component Povarov reaction. Of the synthesized tetrahydroquinoline derivatives, compound 10a displayed the greatest cellular proliferation inhibitory activities with IC50 values of 2.5–16.7 μmol/l. In addition, 10a induced murine C6 glioma cell apoptosis in a dose-dependent manner by up-regulating the expression of Bax, caspase-3, and caspase-9, and by down-regulating Bcl-2. Our findings suggest that these novel compounds have potential as therapeutic agents via inducing mitochondrial apoptosis. |
| Databáze: | OpenAIRE |
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