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Synthesis and evaluation of bis(imino)anthracene derivatives as G-quadruplex ligands.

ABSTRACT: The synthesis of a small number of bis(imino)anthracene derivatives is reported. They were evaluated via NMR for binding efficacy to the G-quadruplex-forming oligonucleotide sequence (TTGGGTT) and show activity against the HeLa cancer cell line. These novel ligands are compared to previously synthesised G-quadruplex ligands that target telomeres and oncogenes.

SUBMITTER: Coban T

PROVIDER: S-EPMC8152782 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature

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Synthesis and evaluation of bis(imino)anthracene derivatives as G-quadruplex ligands.

Coban Tomris T Robertson Cameron C Schwikkard Sianne S Singer Richard R LeGresley Adam A

RSC medicinal chemistry 20210326 5

The synthesis of a small number of bis(imino)anthracene derivatives is reported. They were evaluated <i>via</i> NMR for binding efficacy to the G-quadruplex-forming oligonucleotide sequence (TTGGGTT) and show activity against the HeLa cancer cell line. These novel ligands are compared to previously synthesised G-quadruplex ligands that target telomeres and oncogenes. ...[more]

PMID: 34124673

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