876-30-2

Upstream product

• 880-03-5 4-(methoxymethoxy)-1-nitrobenzene 
• 1124-31-8 potassium 4-nitrophenolate 
• 100-02-7 4-nitro-phenol 
• 1402073-33-9 4'-[(methoxymethyl)oxy]acetanilide 
• 824-91-9 O-methoxymethylphenol 
• 123-30-8 4-amino-phenol 
• 7107-59-7 4-(N-Benzyloxycarbonylamino)phenol 

Downstream Products

• 99284-67-0 N-(3-trimethylsilylprop-2-ynylidene)-4-methoxymethoxyaniline 
• 74015-59-1 [(E)-5,5-Diethoxy-pent-2-en-(Z)-ylidene]-(4-methoxymethoxy-phenyl)-amine 
• 112213-43-1 [4-(tert-Butyl-diphenyl-silanyloxy)-but-2-yn-(E)-ylidene]-(4-methoxymethoxy-phenyl)-amine 
• 213664-72-3 1-N-(3-(3-isopropylureido)benzyl)-3-(3-(4-(methoxymethyloxy)phenyl)thioureido)-2,3,4,5-tetrahydro-1H-1-benzazepin-2-one 
• 767306-82-1 (Z)-2-(2,4-Dichloro-5-fluoro-benzoyl)-3-(4-methoxymethoxy-phenylamino)-acrylic acid methyl ester 
• 402923-38-0 7-chloro-6-fluoro-1-(4-methoxymethoxy-phenyl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid 
• 402923-35-7 7-chloro-6-fluoro-1-(4-methoxymethoxy-phenyl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid methyl ester 
• 402923-40-4 6-fluoro-1-(4-methoxymethoxy-phenyl)-7-(4-methyl-piperazin-1-yl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid 
• 402923-44-8 6-fluoro-1-(4-hydroxy-phenyl)-7-(4-methyl-piperazin-1-yl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid benzyl ester 
• 402923-41-5 6-fluoro-1-(4-methoxymethoxy-phenyl)-7-(4-methyl-piperazin-1-yl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid benzyl ester 
• 402923-45-9 1-[4-(bis-benzyloxy-phosphoryloxy)-phenyl]-6-fluoro-7-(4-methyl-piperazin-1-yl)-4-oxo-1,4-dihydro-quinoline-3-carboxylic acid benzyl ester 
• 213664-73-4 3-(3-(4-hydroxyphenyl)thioureido)-1-N-(3-(3-isopropylureido)benzyl)-2,3,4,5-tetrahydro-1H-1-benzazepin-2-one 
• 211761-71-6 3-(3-(4-hydroxyphenyl)-S-methylphenylisothioureido)-1-N-(3-(3-isopropylureido)benzyl)-2,3,4,5-tetrahydro-1H-1-benzazepin-2-one 
• 99284-70-5 (3RS,4SR)-1-(4-methoxymethoxyphenyl)-3-phenoxyacetamido-4-trimethylsilylethynylazetidin-2-one 

Relevant academic research and scientific papers

Synthesis and Biological Evaluation of Novel Substituted 4-Anilinoquinazolines as Antitumor Agents

Eleven novel 4-anilinoquinazoline derivatives were synthesized and evaluated for their in?vitro antiproliferative activity. Among them, compound 9a exhibited the best potency, with IC50 values of 25?682?nm against various types of cancer cell l

FLUORESCENT SENSORS OF PEROXYNITRITE TARGETED TO THE ENDOPLASMIC RETICULUM

A compound can be a pro-fluorophore peroxynitrite sensor that generates a fluorophore when cleaved by peroxynitrite, having a structure of Formula A: wherein: moiety A is an ER-targeting fluorophore; Y is a linker; and moiety B is a phenol, substituted or

HISTONE DEACETYLASE INHIBITOR, AND PREPARATION METHOD AND USE THEREOF

A compound represented by Formula I or pharmaceutically acceptable salt thereof. The present invention relates to a 4-arylamino quinazoline hydroxamic acid compound having a histone deacetylase inhibitory activity, preparation method of the compound, pharmaceutical composition comprising the compound, and use of the compound and the pharmaceutical composition in the preparation of a histone deacetylase inhibitor medicine. The present invention aims at acquiring, via a medicine design and a synthetic technology, a series of selective histone deacetylase inhibitors having good hypotype selectivity and favorable pharmacokinetic characteristics based on optimization of an enzyme surface recognition region and connection region of 4-arylamino quinazoline, thus reducing an effect on normal tissues or cells while improving an antineoplastic activity of the normal tissues or cells.

Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer

Novel selective histone deacetylase 6 (HDAC6) inhibitors using the quinazoline as the cap were designed, synthesized, and evaluated for HDAC enzymatic assays. N-Hydroxy-4-(2-methoxy-5-(methyl(2-methylquinazolin-4-yl)amino)phenoxy)butanamide, 23bb, was the

A histone deacetylase inhibitor and its preparation and use (by machine translation)

The invention provides a compound of formula I illustrated compound or its pharmaceutically acceptable salt, relates to has the histone deacetylase inhibitory activity of the 4 - aryl amino [...] novel class of compound, the preparation of the compounds, comprising the pharmaceutical composition and the compounds and pharmaceutical compositions in the preparation of histone deacetylase enzyme inhibitor drug in its class of use; aimed at through the drug design and synthesis means based on obtaining a series of 4 - aryl amino [...] surface of the cleat and linkage area optimization, with subtype selective and good medicine generation of dynamics characteristic of selective histone deacetylase inhibitors, in order to improve the anti-tumor activity at the same time to reduce the impact of the normal tissue or cells. (by machine translation)

Site-selective arene C-H amination via photoredox catalysis

Over the past several decades, organometallic cross-coupling chemistry has developed into one of the most reliable approaches to assemble complex aromatic compounds from preoxidized starting materials. More recently, transition metal-catalyzed carbon-hydrogen activation has circumvented the need for preoxidized starting materials, but this approach is limited by a lack of practical amination protocols. Here, we present a blueprint for aromatic carbon-hydrogen functionalization via photoredox catalysis and describe the utility of this strategy for arene amination. An organic photoredox-based catalyst system, consisting of an acridinium photooxidant and a nitroxyl radical, promotes site-selective amination of a variety of simple and complex aromatics with heteroaromatic azoles of interest in pharmaceutical research. We also describe the atom-economical use of ammonia to form anilines, without the need for prefunctionalization of the aromatic component.

PRODUCTION METHOD FOR COMPOUND COMPRISING AMINO GROUP AND/OR HYDROXYL GROUP

Disclosed is a method for producing a compound having an amino group and/or a hydroxyl group from a substrate compound having an atomic group containing CO or CS by eliminating said atomic group. The substrate compound having an atomic group containing CO or CS (for example, an amide, a carbamate, or the like) is allowed to react with a compound expressed by formula (I) below, at a temperature of 120°C or lower, preferably in the presence of an ammonium salt, to eliminate said atomic group containing CO or CS. In formula (I) A may not be present, and in a case where A is present, A represents an alkyl group having 1 to 6 carbon atoms. ????????H2N-A-NH2?????(I)

Bazedoxifene-scaffold-based mimetics of solomonsterols A and B as novel pregnane x receptor antagonists

Pregnane X receptor (PXR), a member of the NR1I nuclear receptor family, acts as a xenobiotic sensor and a paramount transcriptional regulator of drug-metabolizing enzymes and transporters. The overexpression of PXR in various cancer cells indicates the importance of PXR as a drug target for countering multidrug resistance in anticancer treatments. We describe the discovery of novel bazedoxifene-scaffold-based PXR antagonists inspired by the marine sulfated steroids solomonsterol A and B as natural leads. A luciferase reporter assay on a PXR-transfected HepG2 cell line identified compounds 19-24 as promising PXR antagonists. Further structure-activity relationship studies of the most active PXR antagonist from the series (compound 20, IC50 = 11 μM) revealed the importance of hydroxyl groups as hydrogen-bond donors for PXR antagonistic activity. PXR antagonists 20 and 24 (IC50 = 14 μM), in addition to the downregulation of PXR expression, exhibited inhibition of PXR-induced CYP3A4 expression, which illustrates their potential to suppress PXR-regulated phase-I drug metabolism.

Molecular imaging of peroxynitrite with HKGreen-4 in live cells and tissues

Peroxynitrite (ONOO-), the product of a radical combination reaction of nitric oxide and superoxide, is a potent biological oxidant involved in a broad spectrum of physiological and pathological processes. Herein we report the development, characterization, and biological applications of a new fluorescent probe, HKGreen-4, for peroxynitrite detection and imaging. HKGreen-4 utilizes a peroxynitrite-triggered oxidative N-dearylation reaction to achieve an exceptionally sensitive and selective fluorescence turn-on response toward peroxynitrite in chemical systems and biological samples. We have thoroughly evaluated the utility of HKGreen-4 for intracellular peroxynitrite imaging and, more importantly, demonstrated that HKGreen-4 can be efficiently employed to visualize endogenous peroxynitrite generated in Escherichia coli-challenged macrophages and in live tissues from a mouse model of atherosclerosis. This probe should serve as a powerful molecular imaging tool to explore peroxynitrite biology under a variety of physiological and pathological contexts.