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双(亚氨基)蒽衍生物作为G-四链体配体的合成与评价

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

作者信息

Coban Tomris, Robertson Cameron, Schwikkard Sianne, Singer Richard, LeGresley Adam

机构信息

LSP&C, SEC Faculty, Kingston University Kingston-upon-Thames KT1 2EE UK

出版信息

RSC Med Chem. 2021 Mar 26;12(5):751-757. doi: 10.1039/d0md00428f.

Abstract

The synthesis of a small number of bis(imino)anthracene derivatives is reported. They were evaluated 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.

摘要

报道了少量双(亚氨基)蒽衍生物的合成。通过核磁共振对它们与形成G-四链体的寡核苷酸序列(TTGGGTT)的结合效力进行了评估,并且它们对HeLa癌细胞系显示出活性。将这些新型配体与先前合成的靶向端粒和癌基因的G-四链体配体进行了比较。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5852/8152782/7d36d27cd279/d0md00428f-f1.jpg

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