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Amino-Acid-Derived Naphthalenediimides as Versatile G-Quadruplex Binders

DOI: 10.1002/chem.201700957 DOI Help

Authors: Dora M. Răsădean (University of Bath) , Bin Sheng (University of Bath) , Jyotirmayee Dash (Indian Association for the Cultivation of Science) , G. Dan Pantos (University of Bath)
Co-authored by industrial partner: No

Type: Journal Paper
Journal: Chemistry - A European Journal , VOL 23 , PAGES 8491 - 8499

State: Published (Approved)
Published: June 2017
Diamond Proposal Number(s): 10415 , 12668

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.

Journal Keywords: circular dichroism, DNA, G-quadruplex, naphthalenediimide, structure–activity relationships

Subject Areas: Biology and Bio-materials, Medicine, Chemistry


Instruments: B23-Circular Dichroism