53461-08-8

Upstream product

• 66493-39-8 4-(N-tert-butoxycarbonyl)aminobenzoic acid 
• 109-55-7 1-amino-3-(dimethylamino)propane 
• 122-04-3 4-nitro-benzoyl chloride 
• 88452-44-2 N-(3-dimethylamino-propyl)-4-nitro-benzamide 

Downstream Products

• 1310570-13-8 4-(3-chloro-7-methoxyfuro[2,3-b]quinolin-4-ylamino)-N-(3-dimethylaminopropyl)benzamide 
• 1201692-29-6 4-(9-cyclopentyl-7,7-difluoro-6-oxo-5-propyl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl-amino)-N-(3-dimethyl-amino-propyl)-benzamide 
• 1201692-23-0 4-(9-cyclopentyl-5-ethyl-7,7-difluoro-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl-amino)-N-(3-dimethyl-amino-propyl)-benzamide 
• 1201691-23-7 4-(9-cyclobutyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-ylamino)-N-(3-dimethylamino-propyl)-benzamide 
• 1201692-16-1 4-(9-cyclopentyl-7,7-difluoro-6-oxo-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,4]diazepin-2-yl-amino)-N-(3-dimethyl-amino-propyl)-benzamide 
• 466694-49-5 methyl 3-(Z)-[1-{4-[(3-dimethylamino-propyl)-carbamoyl]-phenylamino}-1-phenyl-methylidene]-2-indolinone-6-carboxylate 

Relevant academic research and scientific papers

A platinum(ii) phenylphenanthroimidazole with an extended side-chain exhibits slow dissociation from a c-kit G-quadruplex motif

A series of three platinum(II) phenanthroimidazoles each containing a protonable side-chain appended from the phenyl moiety through copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC) were evaluated for their capacities to bind to human telomere, c-Myc, and c-Kit derived G-quadruplexes. The side-chain has been optimized to enable a multivalent binding mode to G-quadruplex motifs, which would potentially result in selective targeting. Molecular modeling, high-throughput fluorescence intercalator displacement (HT-FID) assays, and surface plasmon resonance (SPR) studies demonstrate that complex 2 exhibits significantly slower dissociation rates compared to platinum phenanthroimidazoles without side-chains and other reported G-quadruplex binders. Complex 2 showed little cytotoxicity in HeLa and A172 cancer cell lines, consistent with the fact that it does not follow a telomere-targeting pathway. Preliminary mRNA analysis shows that 2 specifically interacts with the ckit promoter region. Overall, this study validates 2 as a useful molecular probe for c-Kit related cancer pathways. Bound to impress: A series of three platinum(II) phenanthroimidazoles each containing a protonable side-chain appended from the phenyl moiety through copper(I)-catalyzed azide-alkyne cycloaddition (CuAAC), was evaluated for their capacity to bind to human telomere, c-Myc, and c-Kit derived G-quadruplexes (see scheme). The presence of the side-chain enables a multivalent binding mode to G-quadruplex motifs. Copyright

Aromatic analogues of DNA minor groove binders - Synthesis and biological evaluation

Nine carbocyclic analogues of mono- and bis-lexitropsins and two analogues of pentamidine with unsubstituted N-terminal amine group were synthesized. We have investigated the cytotoxic activity of new aromatic analogues of DNA binding ligands in MCF-7 breast cancer cells and assessed their ability to act as inhibitors of topoisomerase I and II. These studies indicate that aromatic analogues of bis-netropsin contain two identical units tethered by alkyloxyl chains are a potent catalytic inhibitor of both topoisomerases and exhibit moderate cytotoxicity in MCF-7 breast cancer cells.

NOVEL CARBOXAMIDE COMPOUNDS FOR USE IN MCH RECEPTOR RELATED DISORDERS

Novel compounds of formula (I) which modulate MCH activity are disclosed, in which A is a linker; B is a connecting moiety; Ar1 and Ar2 are aryl or heteroaryl groups; R1 and R2 are hydrogen, halogen atoms, CF3, OCF3/