Răsădean, Dora M. ; Sheng, Bin ; Dash, Jyotirmayee ; Pantoş, G. Dan (2017) Amino-Acid-Derived Naphthalenediimides as Versatile G-Quadruplex Binders Chemistry - A European Journal, 23 (35). pp. 8491-8499. ISSN 0947-6539
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Official URL: http://doi.org/10.1002/chem.201700957
Related URL: http://dx.doi.org/10.1002/chem.201700957
Abstract
The design and synthesis of water soluble, amino-acid-functionalised naphthalenediimides (NDIs) as potential ligands of native G-quadruplexes is reported. The NDIs were tested on a panel of oncogene promoters, on the human telomeric sequence h-telo, and on double-stranded DNA. Out of the ligands tested, NDI 3 (Nϵ -Boc-l-lysine NDI) exhibited a highly discriminating nature by only stabilising the oncogene promoter c-kit2, which is up-regulated up to 80 % in ovarian, gastrointestinal, and breast malignancies.
| Item Type: | Article |
|---|---|
| Source: | Copyright of this article belongs to Wiley-VCH Verlag GmbH & Co. |
| Keywords: | DNA; G-quadruplex; Circular dichroism; Naphthalenediimide; Structure-activity relationships. |
| ID Code: | 126626 |
| Deposited On: | 17 Oct 2022 05:45 |
| Last Modified: | 17 Oct 2022 05:45 |
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