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Schultes CM Guyen B Cuesta J Neidle S 《Bioorganic & medicinal chemistry letters》2004,14(16):4347-4351
Telomerase and telomere maintenance are emerging targets for the treatment of human cancers. We report here on the targeting of the telomere-telomerase complex with a series of small molecules based on an acridine platform. A series of 3,6-bisamidoacridines with extended 9-anilino sidechains were designed and synthesised as potential telomeric G-quadruplex DNA (G4) interacting compounds. G4-stabilisation was assessed using a high-throughput FRET (fluorescence resonance energy transfer) assay and telomerase inhibition quantified by a modified TRAP (telomerase repeat amplification protocol) method. Within the series, the compounds showed significant G4-stabilising ability (Delta T(m) values of 25-36 degrees C at 1 microM concentration) and telomerase inhibition in the nanomolar region ((tel)EC(50) values of 80-318 nM). Furthermore, a direct correlation between the FRET and TRAP assays was observed, supporting the use of the rapid screening FRET assay for early assessment of potential G4-stabilising telomerase inhibitors. 相似文献
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Josephine Geertsen Keller Kirstine Mejlstrup Hymller Maria Eriksen Thorsager Noriko
Y Hansen Jens
Uldum Erlandsen Cinzia Tesauro Anne
Katrine
W Simonsen Anne
Bech Andersen Kamilla Vands
Petersen Lise
Lolle Holm Magnus Stougaard Brage
Storstein Andresen Peter Kristensen Rikke Frhlich Birgitta
R Knudsen 《Nucleic acids research》2022,50(11):6332
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