Synthesis and antiproliferative evaluation of novel N-arylquinolones
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Novel N-aryl-substituted quinolones were evaluated for antiproliferative activity. The chemical modifications were inspired by previously reported cytotoxic agents with structural similarities. Dimethylated anilines displayed the most potent effect in the renal cancer cell line Caki-1 and the breast cancer cell line MDA-MB-231, with GI50 values down to 24 µM. Further evaluation in the NCI60 cell lines revealed growth inhibition up to 50%, with the strongest effect observed in renal and lung cancer cell lines. In silico ADMET evaluation indicated favorable characteristics for both gastrointestinal and CNS uptake. The potential toxic electrophilic α,β-unsaturated carbonyl functionalities were shown to be inert to ethanethiol.
KeywordsAntitumor agents Cancer Heterocycles Structure–activity relationships NCI60
The National Cancer Institute is acknowledged for the performed cell line studies. The authors are grateful for support received from the Norwegian Medical Cyclotron Center.
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