Synthesis, cytotoxic activity, DNA binding and molecular docking studies of novel 9-anilinothiazolo[5,4-b]quinoline derivatives

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• 作者：Francisco J. Reyes-Rangel ; A. Kémish López-Rodríguez…
• 关键词：Thiazolo[5 ; 4 ; b]quinoline ; Cytotoxic activity ; DNA intercalators ; Molecular docking
• 刊名：Medicinal Chemistry Research
• 出版年：2016
• 出版时间：December 2016
• 年：2016
• 卷：25
• 期：12
• 页码：2976-2988
• 全文大小：1,507 KB
• 刊物主题：Pharmacology/Toxicology; Biochemistry, general; Cell Biology;
• 出版者：Springer US
• ISSN：1554-8120
• 卷排序：25

文摘

Novel thiazolo[5,4-b]quinoline derivatives were prepared with or without a (2-(azacycloalkyl)ethyl)amino substituent at the 2-position. The effect of the substituent at 2-position on cytotoxic activity, DNA-intercalation and cytotoxic properties were evaluated. Substituents at 2-position bearing an aliphatic amine favored cytotoxicity, while removal of these substituents resulted in low or negligible cytotoxic properties. Additionally, the in silico predicted binding mode of the novel compounds into DNA correlated with the experimental intercalation data. These results suggest a strong influence of the substituent at 2-position on the DNA intercalation properties.