氨基酸衍生萘二酰亚胺作为多功能 G-四链体结合物。
Amino-Acid-Derived Naphthalenediimides as Versatile G-Quadruplex Binders.
机构信息
Department of Chemistry, University of Bath, Claverton Down, Bath, BA2 7AY, UK.
Department of Organic Chemistry, Indian Association for the Cultivation of Science, 2A & @B Raja S C Mullick Road, Kolkata, 700032, India.
出版信息
Chemistry. 2017 Jun 22;23(35):8491-8499. doi: 10.1002/chem.201700957. Epub 2017 May 24.
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 (N -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.
本文报道了具有水溶性和氨基酸官能团的萘二酰亚胺（NDIs）作为天然 G-四链体潜在配体的设计和合成。这些 NDIs 在一组致癌基因启动子、人端粒序列 h-telo 和双链 DNA 上进行了测试。在所测试的配体中，NDI 3（N-Boc-l-赖氨酸 NDI）通过仅稳定上调高达 80%的卵巢、胃肠道和乳腺癌中的致癌基因启动子 c-kit2，表现出高度的选择性。
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