Cytotoxicity Evaluation of Novel bis(2-aminoethyl)amine Derivatives

Seven novel derivatives of bis(2-aminoethyl)amine were synthesized. For compounds and single crystals were isolated and X-ray diffraction experiments were done. Lipophilicity and drug likeness were calculated in the initial stage of research. All compounds were screened for their in vitro cytotoxic...

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Veröffentlicht in:Molecules (Basel, Switzerland) Switzerland), 2020-06, Vol.25 (12), p.2816
Hauptverfasser: Szulczyk, Daniel, Bielenica, Anna, Roszkowski, Piotr, Dobrowolski, Michał A, Olejarz, Wioletta, Napiórkowska, Mariola, Struga, Marta
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Sprache:eng
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Zusammenfassung:Seven novel derivatives of bis(2-aminoethyl)amine were synthesized. For compounds and single crystals were isolated and X-ray diffraction experiments were done. Lipophilicity and drug likeness were calculated in the initial stage of research. All compounds were screened for their in vitro cytotoxic activity against a panel of human cancer cell lines, which is contrary to normal (HaCaT) cell lines, by using the MTT method. Studies were followed by lactate dehydrogenase assay, apoptotic activity, and interleukin-6 assay. Within the studied group, compound showed the most promising results in all biological studies. The strongest influence in A549 cells was denoted for derivative , which inhibited interleukin release almost tenfold, as compared to the control.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules25122816