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Ten novel compounds were evaluated using F\u00f6rster resonance energy transfer (FRET) melting, circular dichroism (CD), and fluorescence spectroscopy on several G4 sequences. Biophysical characterization led to the identification of compounds <jats:bold>4\u2009a<\/jats:bold>, <jats:bold>4\u2009b<\/jats:bold>, and <jats:bold>5\u2009b<\/jats:bold> as good G4 ligands of KRAS G4 sequences. The impact on cell viability of all derivatives was also assessed, revealing weak effects. However, compound <jats:bold>2\u2009a<\/jats:bold> exhibited cytotoxicity activity on A549 and H1299 cancer cells and low cytotoxicity towards MRC\u20105 non\u2010malignant cells MRC\u20105 not connected with its G4\u2010binding ability. Flow cytometry showed that <jats:bold>2\u2009a<\/jats:bold> induced a cell viability decrease in S and G2\/M phases for A549 and H1299; thus, more studies should be performed to explore the proteins involved in cell cycle regulation.<\/jats:p>","DOI":"10.1002\/cmdc.202400591","type":"journal-article","created":{"date-parts":[[2024,11,2]],"date-time":"2024-11-02T05:08:20Z","timestamp":1730524100000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Synthesis of 1,10\u2010Phenanthroline\u20102,9\u2010bistriazoles: Evaluation as G\u2010Quadruplex Binders and Anti\u2010Tumor Activity"],"prefix":"10.1002","volume":"20","author":[{"given":"Joana","family":"Figueiredo","sequence":"first","affiliation":[{"name":"CICS-UBI - Health Sciences Research Centre University of Beira Interior  Av. Infante D. 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