63010-68-4

Basic information

• Product Name: 2-[(2-Fluoro-phenylaMino)-Methylene]-Malonic acid diethyl ester
• Synonyms: 2-[(2-Fluoro-phenylaMino)-Methylene]-Malonic acid diethyl ester;diethyl {[(2-fluorophenyl)amino]methylidene}propanedioate
• CAS NO: 63010-68-4
• Molecular Formula: C₁₄H₁₆FNO₄
• Molecular Weight: 281.2795432
• Mol File: 63010-68-4.mol
• Article Data: 14

Chemical Properties

• Appearance: /
• CAS DataBase Reference: 2-[(2-Fluoro-phenylaMino)-Methylene]-Malonic acid diethyl ester(CAS DataBase Reference)
• NIST Chemistry Reference: 2-[(2-Fluoro-phenylaMino)-Methylene]-Malonic acid diethyl ester(63010-68-4)
• EPA Substance Registry System: 2-[(2-Fluoro-phenylaMino)-Methylene]-Malonic acid diethyl ester(63010-68-4)

Safety Data

• Hazardous Substances Data: 63010-68-4(Hazardous Substances Data)

Upstream product

• 348-54-9 2-Fluoroaniline 
• 87-13-8 diethyl 2-ethoxymethylenemalonate 
• 40131-09-7 diethyl methoxymethylenemalonate 
• 105-53-3 diethyl malonate 

Downstream Products

• 63010-69-5 ethyl 8-fluoro-4-hydroxy-3-quinolinecarboxylate 
• 1435910-89-6 ethyl 8-fluoro-1-(oxiran-2-ylmethyl)-4-oxo-1,4-dihydroquinoline-3-carboxylate 
• 1414879-48-3 8-SH-3-CONHBn-quinoline 
• 56824-90-9 4-chloro-8-fluoro-quinoline-3-carboxylic acid ethyl ester 
• 1207748-36-4 ethyl N-benzyl-8-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylate 
• 63010-70-8 8-Fluoro-4-hydroxyquinoline-3-carboxylic acid 
• 71082-99-0 8-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 
• 71083-06-2 ethyl 8-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylate 

Relevant articles and documents

3-(Benzo[: D] thiazol-2-yl)-4-aminoquinoline derivatives as novel scaffold topoisomerase i inhibitor via DNA intercalation: Design, synthesis, and antitumor activities

Twenty-seven 3-(benzo[d]thiazol-2-yl)-4-aminoquinoline derivatives have been designed and synthesized as topoisomerase I inhibitors. The in vitro anti-proliferation evaluation against four human cancer cell lines (MGC-803, HepG-2, T24, and NCI-H460) and one normal cell line (HL-7702) indicated that most of them exhibited potent cytotoxicity. Among them, 5a was identified as the most promising candidate with a low IC50 value of about 2.20 ± 0.14 and was selected for further exploration. Spectroscopic analyses and agarose-gel electrophoresis assays indicated that 5a could interact with DNA and strongly inhibit topoisomerase I (Topo I). Further screening of the Topo I activity of compounds 5b, 5c, 5e, 5f, 5h, 5i, 5j, 5l, and 5n suggested that some of the compounds might exert quite a different cytotoxicity profile to that of 5a. Molecular modeling studies confirmed that 5a adopts a unique mode to interact with DNA and Topo I. Other molecular mechanistic studies suggested that the treatment of MGC-803 cells with 5a induces S phase arrest, up-regulates the pro-apoptotic protein, down-regulates the anti-apoptotic protein, activates caspase-3, and subsequently induces mitochondrial dysfunction so as to induce cell apoptosis. The in vivo efficiency of 5a was also evaluated on MGC-803 xenograft nude mice and the relative tumor growth inhibition was 42.4percent at 12 mg kg-1 without an obvious loss in the body weight. This journal is

Synthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer's disease therapies

In present study a series of triazolopyrimidine-quinoline and cyanopyridine-quinoline hybrids were designed, synthesized and evaluated as acetylcholinesterase inhibitors (AChEIs). Molecular docking and scoring was utilized for the design of inhibitors. The molecules were synthesized via an easily accessible, convergent synthetic route. Three triazolopyrimidine based compounds showed nanomolar activity towards acetylcholinesterase. Among them, Ethyl 6-fluoro-4-(4-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperazin-1-yl)quinoline-3-carboxylate (10d), strongly inhibited AChE with IC50 value of 42 nM. Furthermore compound 10d was identified as most promising compound with 12 fold selectivity against butyrylcholinesterase (BuChE). This compound displayed a composed multitargeted profile with promising inhibition of self-induced and AChE - induced Aβ aggregation and antioxidant activity.

COMPOSITIONS AND METHODS FOR JAMM PROTEIN INHIBITION

Compounds, pharmaceutical compositions, and methods of using such compounds to treat or prevent diseases or disorders associated with or mediated by JAMM proteins are disclosed.