Synthesis, Biological Evaluation and Stability Studies of Some Novel Aza-Acridine Aminoderivatives.

Maria Karelou, Vasileios Kourafalos, Athanasia P Tragomalou, Panagiotis Marakos, Nicole Pouli, Ourania E Tsitsilonis, Evangelos Gikas, Ioannis K Kostakis

Molecules (Basel, Switzerland) 2020 Oct 08

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Several new amino-substituted aza-acridine derivatives bearing a basic side chain have been designed and synthesized. The antiproliferative activity of the target compounds has been evaluated against three cancer cell lines-namely HCT-116 (colorectal), the uterine sarcoma MES-SA, and its doxorubicin-resistant variant MES-SA/Dx5. A limited number of the new acridines showed marginal cytotoxicity against the tested cell lines; nevertheless, these analogues possessed a similar substitution pattern. The moderate biological activity of these derivatives was attributed to their instability in aqueous media, which has been studied by mass spectrometry and computational chemistry experiments at the density functional level of theory (DFT).

Citation

Maria Karelou, Vasileios Kourafalos, Athanasia P Tragomalou, Panagiotis Marakos, Nicole Pouli, Ourania E Tsitsilonis, Evangelos Gikas, Ioannis K Kostakis. Synthesis, Biological Evaluation and Stability Studies of Some Novel Aza-Acridine Aminoderivatives. Molecules (Basel, Switzerland). 2020 Oct 08;25(19)