New highly hydrosoluble and not self-aggregated perylene derivatives with three and four polar side-chains as G-quadruplex telomere targeting agents and telomerase inhibitors

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• 作者：Marco Franceschin ; Emanuela Pascucci ; Antonello Alvino ; Danilo D’ ; Ambrosio ; Arm ; odoriano Bianco ; Giancarlo Ortaggi ; Maria Savino
• 关键词：Hydrosoluble perylene derivatives ; G-quadruplex ; Telomerase inhibitors
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 出版时间：1 May 2007
• 年：2007
• 卷：17
• 期：9
• 页码：2515-2522
• 全文大小：1678 K

文摘

Four new perylene derivatives with three and four basic side-chains are reported here as G-quadruplex interactive compounds. The new perylene derivatives are readily soluble in water and not self-aggregated, in contrast to what happens with the previously reported two side-chain perylene derivatives. All four compounds are able to induce the G-quadruplex and to inhibit 50 % of telomerase activity at about 5 μM concentration, showing a similar efficiency with respect to each other. Molecular modelling studies are presented to try to explain these findings.