Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3H)-Ones with Antiproliferative Activities

Sixteen new 2-substituted quinazolines were synthesized using a straightforward methodology starting from 2-methoxybezoic acid or 3-methoxy-2-naphthoic acid. The anti-proliferative activity of the target compounds was evaluated against nine cancer cell lines. Additionally, all the compounds were scr...

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Veröffentlicht in:MOLECULES 2023-12, Vol.28 (23)
Hauptverfasser: Karelou, Maria, Kampasis, Dionysis, Kalampaliki, Amalia D, Persoons, Leentje, Kraemer, Andreas, Schols, Dominique, Knapp, Stefan, De Jonghe, Steven, Kostakis, Ioannis K, Nikolaropoulos, Sotiris S
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Sprache:eng
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Zusammenfassung:Sixteen new 2-substituted quinazolines were synthesized using a straightforward methodology starting from 2-methoxybezoic acid or 3-methoxy-2-naphthoic acid. The anti-proliferative activity of the target compounds was evaluated against nine cancer cell lines. Additionally, all the compounds were screened for their potency and selectivity against a panel of 109 kinases and four bromodomains, using Differential Scanning Fluorimetry (DSF). Compound 17 bearing a 2-methoxyphenyl substitution along with a basic side chain displayed a remarkable profile against the majority of the tested cell lines.
ISSN:1420-3049
1420-3049