851651-86-0

Upstream product

• 99-09-2 3-nitro-aniline 
• 123-75-1 pyrrolidine 
• 625-36-5 2-chloropropionyl chloride 
• 60284-53-9 3-chloro-N-(3-nitrophenyl)propanamide 

Downstream Products

• 1070978-77-6 N-(3-azidophenyl)-3-(pyrrolidin-1-yl)propanamide 
• 1446421-10-8 N-(3-(3-(4-(bis(2-chloroethyl)amino)phenyl)ureido)phenyl)-3-(pyrrolidin-1-yl)propanamide 
• 1070978-30-1 5,5'-ureylene-di-(1-(3-(3-(pyrrolidin-1-yl)propanamido)-phenyl)-3-phenylurea) 
• 1070978-46-9 1,3-bis(4-(1-(3-(3-(pyrrolidin-1-yl)propanamido)phenyl)-1H-1,2,3-triazol-4-yl)phenyl)urea 
• 1070977-78-4 1,3-bis(3-(3-(3-(pyrrolidin-1-yl)propanamido)phenylcarbamoyl)phenyl)urea 
• 1070977-92-2 1,3-bis(4-(3-(3-(pyrrolidin-1-yl)propanamido)phenylcarbamoyl)phenyl)urea 
• 1070978-36-7 1-(3-(1-(3-(3-(pyrrolidin-1-yl)propanamido)phenyl)-1H-1,2,3-triazol-4-yl)phenyl)-3-(3-(1-(3-(acrylamido)phenyl)-1H-1,2,3-triazol-4-yl)phenyl)urea 
• 1070978-34-5 1,3-bis(3-(1-(3-(3-(pyrrolidin-1-yl)propanamido)phenyl)-1H-1,2,3-triazol-4-yl)phenyl)urea 
• 1070978-04-9 N-(3-(3-(pyrrolidin-1-yl)propanamido)phenyl)-2-(1,2-dihydro-2,4-dioxoquinazolin-3(4H)-yl)benzamide 
• 1070979-17-7 1-(3-(3-(pyrrolidin-1-yl)propanamido)phenyl)-3-(3-nitrophenyl)urea 
• 1070979-19-9 1-(3-(3-(pyrrolidin-1-yl)propanamido)phenyl)-3-(3-aminophenyl)urea 
• 851651-87-1 N-(3-aminophenyl)-3-(pyrrolidin-1-yl)propanamide 

Relevant academic research and scientific papers

Design and synthesis of potent antitumor water-soluble phenyl N-mustard-benzenealkylamide conjugates via a bioisostere approach

A series of new, water-soluble phenyl N-mustard-benzenealkylamide conjugates containing hydrophilic ω-dialkylaminoalkylamide or ω-cyclic aminoalkylamide moieties were synthesized via a bioisostere approach. These compounds have a broad spectrum of antitumor activity against a panel of human tumor cell lines. Of these derivatives, compound 18b effectively suppressed the growth of colon cancer (HCT-116), prostate cancer (PC3), and lung cancer (H460) xenografts. The growth of HCT-116 xenografts was almost completely suppressed when co-treated with compound 18b and 5-fluorouracil. Furthermore, compound 18b can induce DNA cross-linking and cell-cycle arrest at the G2/M phase. Early preclinical studies, including pharmacokinetics in rats, inhibition of the hERG, and 14 days of acute intravenous injection toxicity, suggest that compound 18b is a promising candidate for further preclinical studies.

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.

Design, synthesis and evaluation of 4,5-di-substituted acridone ligands with high G-quadruplex affinity and selectivity, together with low toxicity to normal cells

A series of 4,5-di-substituted acridones have been designed and synthesized. Several compounds show high affinity for telomeric G-quadruplex DNA in classical and competition FRET assays, together with low duplex DNA affinity, although they do not show activity in a telomerase assay or evidence of telomere shortening. They have low toxicity against a panel of cancer cell lines and a normal human fibroblast line, and produce potent senescence-based long-term growth arrest in the MCF7 and A549 cancer cell lines.

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.

Thiazolidinones, their production and use as pharmaceutical agents

Thiazolidinones of general formula I in which Q, A, B, X, R1 and R2 have the meanings that are indicated in the description, as well as those of general formula IA in which Q, A, B, X, R1 and R2a have the meanings that are indicated in the description, their production and use as inhibitors of the polo-like kinase (PLK) for treating various diseases as well as intermediate products for the production of thiazolidinones are described.