Cyclic ferrocenylnaphthalene diimide derivative as a new class of G-quadruplex DNA binding ligand

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• 作者：Md. Monirul Islam^a ; Shinobu Sato^a ; ^b ; Shingo Shinozaki^a ; Shigeori Takenaka^a ; ^b ; ^{shige@che.kyutech.ac.jp}
• 关键词：Cyclic ferrocenylnaphthalene diimide ; Tetraplex DNA binder ; G-quadruplex DNA ; Human telomere DNA ; Promotor region ; Thrombin binding aptamer ; Double stranded DNA
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 January 2017
• 年：2017
• 卷：27
• 期：2
• 页码：329-335
• 全文大小：1366 K
• 卷排序：27

文摘

Cyclic ferrocenylnaphthalene diimide (cFND, 1) was synthesized as G-quadruplex (G4) DNA binder. Compound 1 showed higher binding affinity to G4 than the non-cyclic ferrocenylnaphthalene diimide (FNDI, 2) did. Compound 1 shows 50-times higher binding affinity to G4 DNAs than to double-stranded DNA (dsDNA). G4 DNA structures are more thermally stabilized than dsDNA are by 1. Compound 1 inhibited telomerase activity with an IC50 of 0.4 μM.