891855-91-7

Upstream product

• 10147-71-4 2-chloro-N-(3-nitrophenyl)acetamide 
• 99-09-2 3-nitro-aniline 
• 882340-56-9 N-(3-nitrophenyl)-2-(pyrrolidin-1-yl)acetamide 

Downstream Products

• 1070977-90-0 1,3-bis(4-(3-(2-(pyrrolidin-1-yl)acetamido)phenylcarbamoyl)phenyl)urea 
• 1070978-02-7 N-(3-(2-(pyrrolidin-1-yl)acetamido)phenyl)-2-(1,2-dihydro-2,4-dioxoquinazolin-3(4H)-yl)benzamide 
• 1070977-76-2 1,3-bis(3-(3-(2-(pyrrolidin-1-yl)acetamido)phenylcarbamoyl)phenyl)urea 
• 1262546-38-2 N-(3-azidophenyl)-2-(pyrrolidin-1-yl)acetamide 
• 1262546-39-3 C₄₈H₅₁N₁₅O₃ 
• 1400645-91-1 C₃₈H₃₈N₁₀O₂ 

Relevant academic research and scientific papers

A novel series of G-quadruplex ligands with selectivity for HIF-expressing osteosarcoma and renal cancer cell lines

A series of naphthalene derivatives with disubstituted triazole side-arms have been assembled by click chemistry. Lead compounds show a high level of selectivity for renal, osteo- and Ewing's sarcomas that express the HIF-1α transcription factor. They also interact selectively with the quadruplex DNAs located in the promoter of the HIF genes and it is suggested that the mechanism of action involves inhibition of transcription by drug-mediated quadruplex stabilization in these regions.

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.

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.

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.

Metasubstituted thiazolidinones, their manufacture and use as a drug

This invention involves thiazolidinone of general formula (I) and its creation and use as inhibitors of polo like kinase (PLK) for the treatment of various diseases.