5502-65-8

Upstream product

• 851435-89-7 N-(4-nitro-phenyl)-adipamic acid methyl ester 
• 124-04-9 Adipic acid 
• 100-01-6 4-nitro-aniline 
• 2035-75-8 adipic anhydride 
• 35444-44-1 methyl adipoyl chloride 

Downstream Products

• 754227-35-5 hexanedioic acid (4-amino-phenyl)-amide (6-diethylamino-hexyl)-amide 
• 754227-34-4 hexanedioic acid (4-amino-phenyl)-amide (2-diethylamino-ethyl)-amide 
• 754227-33-3 6-(4-methyl-piperazin-1-yl)-6-oxo-hexanoic acid (4-amino-phenyl)-amide 
• 754227-32-2 6-morpholin-4-yl-6-oxo-hexanoic acid (4-amino-phenyl)-amide 

Relevant academic research and scientific papers

Synthesis, biophysical and biological evaluation of 3,6-bis-amidoacridines with extended 9-anilino substituents as potent G-quadruplex-binding telomerase inhibitors

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 (ΔT m values of 25-36°C at 1μM concentration) and telomerase inhibition in the nanomolar region (telEC50 values of 80-318nM). 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.