851651-89-3

Upstream product

• 851651-88-2 N-(3-nitrophenyl)-4-(pyrrolidin-1-yl)butanamide 
• 99-09-2 3-nitro-aniline 
• 304684-54-6 4-chloro-N-(3-nitrophenyl)butanamide 

Downstream Products

• 1070978-84-5 N-(3-azidophenyl)-4-(pyrrolidin-1-yl)butanamide 
• 1070977-95-5 1,3-bis(4-(3-(4-(pyrrolidin-1-yl)butanamido)phenylcarbamoyl)phenyl)urea 
• 1070978-04-9 N-(3-(3-(pyrrolidin-1-yl)propanamido)phenyl)-2-(1,2-dihydro-2,4-dioxoquinazolin-3(4H)-yl)benzamide 
• 1070977-80-8 1,3-bis(3-(3-(4-(pyrrolidin-1-yl)butanamido)phenylcarbamoyl)phenyl)urea 
• 1262546-41-7 C₅₄H₆₃N₁₅O₃ 
• 1070978-52-7 1,3-bis-(2-(1-(3-(4-(pyrrolidin-1-yl)butanamido)phenyl)-1H-1,2,3-triazol-4-yl)phenyl)urea 
• 1070978-40-3 1,3-bis(3-(1-(3-(4-(pyrrolidin-1-yl)butanamido)phenyl)-1H-1,2,3-triazol-4-yl)phenyl)urea 
• 1070978-49-2 1,3-bis(4-(1-(3-(4-(pyrrolidin-1-yl)butanamido)phenyl)-1H-1,2,3-triazol-4-yl)phenyl)urea 
• 1070978-06-1 N-(3-(4-(pyrrolidin-1-yl)butanamido)phenyl)-2-(1,2-dihydro-2,4-dioxoquinazolin-3(4H)-yl)benzamide 

Relevant academic research and scientific papers

Structure-based design of selective high-affinity telomeric quadruplex-binding ligands

A library of triazole-based telomeric quadruplex-selective ligands has been developed that mimic an established family of tri-substituted acridine-based ligands, using crystal structure data as a starting-point for computer-based design. Binding affinities, estimated by electrospray mass spectrometry, are in accord with the design concept.

UREYLENE DERIVATIVES

The invention concerns compounds of Formula (I) or a salt, solvate or pro-drug thereof. The compounds may be used in therapy, particularly anti-cancer therapy.

Rational design of substituted diarylureas: A scaffold for binding to G-quadruplex motifs

The design and synthesis of a series of urea-based nonpolycyclic aromatic ligands with alkylaminoanilino side chains as telomeric and genomic G-quadruplex DNA interacting agents are described. Their interactions with quadruplexes have been examined by means of fluorescent resonance energy transfer melting, circular dichroism, and surface plasmon resonance-based assays. These validate the design concept for such urea-based ligands and also show that they have significant selectivity over duplex DNA, as well as for particular G-quadruplexes. The ligand-quadruplex complexes were investigated by computational molecular modeling, providing further information on structure-activity relationships. Preliminary biological studies using short-term cell growth inhibition assays show that some of the ligands have cancer cell selectivity, although they appear to have low potency for intracellular telomeric G-quadruplex structures, suggesting that their cellular targets may be other, possibly oncogene-related quadruplexes.

Click chemistry assembly of G-quadruplex ligands incorporating a diarylurea scaffold and triazole linkers

A series of diarylurea ligands were designed to interact selectively with G-quadruplexes and were synthesised using copper(I) catalysed 'click' chemistry to incorporate the 1,4-substituted 1,2,3-triazole ring into the core of the ligands; the optimal ligands demonstrate a high degree of selective telomeric G-quadruplex stabilisation and are not cytotoxic in several cancer cell lines. The Royal Society of Chemistry.