Influence of core extension and side chain nature in targeting G-quadruplex structures with perylene monoimide derivatives

نویسندگان

چکیده

A structure–activity relationship (SAR) study in terms of G-quadruplex binding ability and antiproliferative activity six fluorescent perylenemonoimide (PMIs) derivatives is reported. positive charge seems to be the key target G4. This also reveals importance element substitution potential biological PMIs, being polyethylene glycol (PEG) chains peri position responsible for their activity. Among them, cationic PMI6 with two PEG most promising compound since its fluorescence enhanced presence structures. Moreover, binds human telomeric hTelo high affinity displays a towards HeLa (cervical adenocarcinoma), A549 (lung adenocarcinoma) A2780 (ovarian cells. Its fate can followed inside cells thanks properties: found accumulate mitochondria.

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ژورنال

عنوان ژورنال: Bioorganic Chemistry

سال: 2021

ISSN: ['1090-2120', '0045-2068']

DOI: https://doi.org/10.1016/j.bioorg.2021.104660