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Synthesis and anticancer activity evaluation of some new derivatives of 2-(4-benzoyl-1-piperazinyl)-quinoline and 2-(4-cinnamoyl-1-piperazinyl)-quinoline.

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Kubica K. P., Taciak P. P., Czajkowska A., Sztokfisz-Ignasiak A., Wyrebiak R., Podsadni P., Mlynarczuk-Bialy I., Malejczyk J., Mazurek A. P.
Acta Poloniae Pharmaceutica - Drug Research
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2018
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vol. 75
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issue 4
891-901
EN
In this study we designed and synthesized twenty new derivatives of 2-(4-benzoyl-1-piperazinyl)-quinoline and 2-(4-cinnamoyl-1-piperazinyl)-quinoline with potential anticancer activity. The structures of synthesized compounds were confirmed by 1H and 13C NMR spectroscopy and MS spectrometry. The activity of novel compounds was evaluated in the cell viability assay as well as in the wound healing assay. Presented data show that examined substances have anticancer activity in cell culture. Seven compounds which showed a high rate of cell growth inhibition were selected for further studies. Three of them strongly reduced growth of B16F10 cells. The novel compounds constitute a good base for further studies and optimization of structure for new therapeutically effective anti-cancerous drugs.
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Synthesis and anticancer activity evaluation of novel derivatives of 7-amino-4-methylquinolin-2(1H)-one

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Kubica K. P., Taciak P. P., Czajkowska A., Sztokfisz-Ignasiak A., Wyrebiak R., Mlynarczuk-Bialy I., Malejczyk J., Mazurek A. P.
Acta Poloniae Pharmaceutica - Drug Research
|
2018
|
vol. 75
|
issue 4
903-910
EN
In this study we designed and synthesized sixteen new derivatives of 7-amino-4-methylquinolin-2(1H)-one with potential anticancer activity. The structures of synthesized compounds were confirmed by 1H and 13C NMR. The activity of novel substances was evaluated by cell viability assay and wound healing assay. In vitro tests for series of sixteen novel compounds were performed. The results showed that examined compounds are selective for cancer cells, but their activity for various types of cancer is different. Three of new compounds presented ability to inhibit cells migration. The novel compounds constitute a good starting point for further studies and optimization of structure for new therapeutically effective anti-cancerous drugs. Seven compounds, which showed the highest rate of cell inhibition, were selected for further studies.
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