Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents

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• 作者：Cristina Martins ; Mekala Gunaratnam ; John Stuart ; Vaidahi Makwana ; Olga Greciano ; Anthony P. Reszka ; Lloyd R. Kell ; ; Stephen Neidle
• 关键词：G-quadruplex ; Acridines ; Telomerase
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 April 2007
• 卷：17
• 期：8
• 页码：2293-2298
• 文件大小：1061 K

摘要

The design, synthesis, biophysical and biochemical evaluation is presented of a new series of benzylamino-substituted acridines as G-quadruplex binding telomerase inhibitors. Replacement of the previously reported anilino substituents by benzylamino groups results in enhanced quadruplex interaction, and for one compound, superior telomerase inhibitory activity.