Synthesis and antiproliferative activity of some novel benzo-fused imidazo[1,8]naphthyridinones

Giannouli, Vassiliki; Kostakis, Ioannis K.; Pouli, Nicole; Marakos, Panagiotis; Samara, Pinelopi; Tsitsilonis, Ourania E.

doi:10.1016/j.bmcl.2015.04.093

Cited by 2 publications

(1 citation statement)

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“…The in vitro antiproliferative activities of the new aza-acridine aminoderivatives were evaluated against three human tumor cell lines—namely, HCT-116 (colorectal), the uterine sarcoma MES-SA and its variant MES-SA/Dx5, reported to be 100 times more resistant to doxorubicin (Dx) [ 24 ]. The results of the MTT dye reduction assay, expressed as 50% inhibitory concentrations (IC 50 ) in μM, are summarized in Table 1 .…”

Section: Resultsmentioning

confidence: 99%

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

et al. 2020

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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).

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Section: Resultsmentioning

confidence: 99%