21597-54-6

Upstream product

• 67-56-1 methanol 
• 53653-44-4 2H-Naphtho<2,3-e>-1,3-oxazin-2,4(3H)-dion 
• 5959-52-4 2-Amino-3-naphthoic acid 
• 77-76-9 2,2-dimethoxy-propane 
• 29753-32-0 2H-naphth<2,3-d><3,1>oxazine-2,4(1H)-dione 
• 92-70-6 3-Hydroxy-2-naphthoic acid 
• 18107-18-1 diazomethyl-trimethyl-silane 
• 186581-53-3 diazomethane 

Downstream Products

• 47644-69-9 dimethyl 2,2'-dihydroxy-1,1'-binaphthalene-3,3'-dicarboxylate 
• 141281-58-5 3-Amino-2-(hydroxymethyl)naphthalene 
• 4488-22-6 1,1'-binaphthalene-2,2'-diamine 
• 602-09-5 1,1'-bi-2-naphthol 
• 675578-50-4 N-p-toluenesulfonyl-2-aminonaphthalene-3-carboxylic acid methyl ester 
• 773071-66-2 3-(3-chloromethylbenzoylamino)-naphthalene-2-carboxylic acid methyl ester 
• 144267-76-5 2-phenyl-3-palmitoyloxy-3,4-dihydro--benzoquinazoline-4-thione 
• 144267-77-6 2-phenyl-3-pentadecylthio--benzoquinazoline 
• 144267-75-4 2-phenyl-3-hydroxy-3,4-dihydro--benzoquinazoline-4-thione 
• 144267-74-3 2-phenyl--naphthothiazine-4-thione 
• 402822-79-1 N-allyl-N-(p-toluenesulfonyl)-2-amino-3-ethenylnaphthalene 
• 675578-52-6 N-allyl-N-(p-toluenesulfonyl)-2-amino-3-formylnaphthalene 
• 675578-51-5 N-(p-toluenesulfonyl)-2-amino-3-hydroxymethylnaphthalene 
• 34161-90-5 N-(3-formylnaphthalen-2-yl)-4-methylbenzenesulfonamide 

Relevant academic research and scientific papers

Improving the fluorescent probe acridonylalanine through a combination of theory and experiment

Acridonylalanine (Acd) is a useful fluorophore for studying proteins by fluorescence spectroscopy, but it can potentially be improved by being made longer wavelength or brighter. Here, we report the synthesis of Acd core derivatives and their photophysical characterization. We also performed ab initio calculations of the absorption and emission spectra of Acd derivatives, which agree well with experimental measurements. The amino acid aminoacridonylalanine (Aad) was synthesized in forms appropriate for genetic incorporation and peptide synthesis. We show that Aad is a superior F?rster resonance energy transfer acceptor to Acd in a peptide cleavage assay and that Aad can be activated by an aminoacyl tRNA synthetase for genetic incorporation. Together, these results show that we can use computation to design enhanced Acd derivatives, which can be used in peptides and proteins.

The synthesis of a linear Troeger's base derived from naphthalene: 7H-15H-6,14-methanodinaphtho[2,3-b:2′,3′-f][1,5]diazocine

(Chemical Equation Presented) The title compound 3 was prepared in four steps from commercial 3-amino-2-naphthoic acid in an overall 75 % yield. Attempts to use the same approach in the case of 2-aminonicotinic acid methyl ester failed. All the compounds were characterized by NMR.

Chiroptical sensing of amino acids by stereodynamic imprinting into the ZnII-Complex generating a dihedral chirality

A stereodynamic chiroptical sensor based on three-component assembly of 3-(di-2-picolylaminoacetamido)-2-formyl-naphthalene (1), ZnII and amino acids was developed. The imine formed between 1 and an amino acid has six coordination sites to bind

TARGETED RADIOPHARMACEUTICALS FOR THE DIAGNOSIS AND TREATMENT OF PROSTATE CANCER

A compound of general formula (I): wherein: n is 1, 2 or 3; R1, R2, R3 and R4, independently represent OH or Q; and 20 Q represents a tissue-targeting moeity selected from the group consisting of or a stereoisomer, a hydrate, a solvate, or a salt thereof, or a mixture of same, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said 25 compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of soft tissue diseases, as a sole agent or in combination with other active ingredients.

Halogen-substituted anthranilic acid derivatives provide a novel chemical platform for androgen receptor antagonists

Androgen receptor (AR) antagonists are used for hormone therapy of prostate cancer (PCa). However resistance to the treatment occurs eventually. One possible reason is the occurrence of AR mutations that prevent inhibition of AR-mediated transactivation by antagonists. To offer in future more options to inhibit AR signaling, novel chemical lead structures for new AR antagonists would be beneficial. Here we analyzed structure-activity relationships of a battery of 36 non-steroidal structural variants of methyl anthranilate including 23 synthesized compounds. We identified structural requirements that lead to more potent AR antagonists. Specific compounds inhibit the transactivation of wild-type AR as well as AR mutants that render treatment resistance to hydroxyflutamide, bicalutamide and the second-generation AR antagonist enzalutamide. This suggests a distinct mode of inhibiting the AR compared to the clinically used compounds. Competition assays suggest binding of these compounds to the AR ligand binding domain and inhibit PCa cell proliferation. Moreover, active compounds induce cellular senescence despite inhibition of AR-mediated transactivation indicating a transactivation-independent AR-pathway. In line with this, fluorescence resonance after photobleaching (FRAP) - assays reveal higher mobility of the AR in the cell nuclei. Mechanistically, fluorescence resonance energy transfer (FRET) - assays indicate that the amino-carboxy (N/C)-interaction of the AR is not affected, which is in contrast to known AR-antagonists. This suggests a mechanistically novel mode of AR-antagonism. Together, these findings indicate the identification of a novel chemical platform as a new lead structure that extends the diversity of known AR antagonists and possesses a distinct mode of antagonizing AR-function.

Fused cyclic compound and organoelectroluminescent device comprising the compound

PURPOSE: A condensed cyclic compound is provided to drive an organic electroluminescent device at low voltage and to improve brightness and economic efficiency. CONSTITUTION: A condensed cyclic compound is denoted by chemical formula 1. An organic electroluminescence device comprises an anode, a cathode, and a layer containing the condensed cyclic compounds, placed between the anode and the cathode. A light emitting layer between the anode and the cathode contains the condensed cyclic compounds. The organic electroluminescent device further comprises one or more layers selected among a hole injection layer, a hole transport layer, an electron blocking layer, a hole blocking layer, an electron transport layer, and an electron injection layer.

Amphipathic sulfonamidobenzamides mimicking small antimicrobial marine natural products; investigation of antibacterial and anti-biofilm activity against antibiotic resistant clinical isolates

There is an urgent need for novel antimicrobial agents to address the threat of bacterial resistance to modern society. We have used a structural motif found in antimicrobial marine hit compounds as a basis for synthesizing a library of antimicrobial sulf

Design and synthesis of benzoacridines as estrogenic and anti-estrogenic agents

Estrogens play undisputedly important physiological roles, but lifetime exposure to estrogens has also been linked to the development of breast cancer. Moreover, imbalanced estrogen levels have been associated with various symptoms such as osteoporosis and menopausal disorders. For the improvement of such estrogen imbalances, estrogenic reagents with regulatory properties have shown promising potential. Herein, we report the construction of a 12-arylbenzoacridine library via a diversity-oriented strategy that furnished non-toxic estrogenic and anti-estrogenic agents. Derivatives with a hydroxy group at the molecular edge exhibit potent binding affinity to the estrogen receptor α (ERα) and ERβ (IC50 μM), while binding to the estrogen-related receptor γ (ERRγ), i.e., an orphan nuclear receptor on which estrogens often trigger unfavorable events, was not observed. These findings offer valuable insights into 12-arylbenzoacridines as a novel platform for the development of selective estrogen-receptor modulators (SERMs).

Insights into the myosin II inhibitory potency of A-ring-modified (S)-blebbistatin analogs

Myosin II is an interesting target for therapeutic intervention, as it is involved in a large number of motility-based diseases. (S)-Blebbistatin is a known micromolar inhibitor of this protein. A new series of (S)-blebbistatin derivatives with a modified

CONDENSED CYCLIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

An organic light-emitting device includes: a first electrode; a second electrode facing the first electrode; and an organic layer between the first electrode and the second electrode, the organic layer including an emission layer, wherein the organic laye