Category: quinoxaline

Jo, Hakryul; Patterson, Victoria; Stoessel, Sean; Kuan, Chia-Yi; Hoh, Josephine published the artcile< Protoporphyrins enhance oligomerization and enzymatic activity of HtrA1 serine protease>, Related Products of 163769-88-8, the main research area is protoporphyrin oligomerization HtrA1 serine protease protoporphyria hemin.

High temperature requirement protein A1 (HtrA1), a secreted serine protease of the HtrA family, is associated with a multitude of human diseases. However, the exact functions of HtrA1 in these diseases remain poorly understood. We seek to unravel the mechanisms of HtrA1 by elucidating its interactions with chem. or biol. modulators. To this end, we screened a small mol. library of 500 bioactive compounds to identify those that alter the formation of extracellular HtrA1 complexes in the cell culture medium. An initial characterization of two novel hits from this screen showed that protoporphyrin IX (PPP-IX), a precursor in the heme biosynthetic pathway, and its metalloporphyrin (MPP) derivatives fostered the oligomerization of HtrA1 by binding to the protease domain. As a result of the interaction with MPPs, the proteolytic activity of HtrA1 against Fibulin-5, a specific HtrA1 substrate in age-related macular degeneration (AMD), was increased. This phys. interaction could be abolished by the missense mutations of HtrA1 found in patients with cerebral autosomal recessive arteriopathy with subcortical infarcts and leukoencephalopathy (CARASIL). Furthermore, knockdown of HtrA1 attenuated apoptosis induced by PPP-IX. These results suggest that PPP-IX, or its derivatives, and HtrA1 may function as co-factors whereby porphyrins enhance oligomerization and the protease activity of HtrA1, while active HtrA1 elevates the pro-apoptotic actions of porphyrin derivatives Further anal. of this interplay may shed insights into the pathogenesis of diseases such as AMD, CARASIL and protoporphyria, as well as effective therapeutic development.

PLoS One published new progress about Age-related macular degeneration. 163769-88-8 belongs to class quinoxaline, and the molecular formula is C22H21N3O2, Related Products of 163769-88-8.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Harms, Arthur E. published the artcile< An Efficient Synthesis of 2-Quinoxalinecarboxylic Acid>, Application In Synthesis of 5182-90-1, the main research area is fructose cyclocondensation phenylenediamine; phenylenediamine cyclocondensation monosaccharide; quinoxalinecarboxylic acid preparation.

Development of a cost efficient and scaleable process for 2-quinoxalinecarboxylic acid is described. The primarily goals of the development work were to improve the overall yield of the process, to minimize the use of environmentally unacceptable materials, and to obtain a material with a high level of purity. A variety of approaches were examined, and the most efficient method was a condensation of o-phenylenediamine with a monosaccharide followed by a mild peroxide oxidation

Organic Process Research & Development published new progress about Green chemistry. 5182-90-1 belongs to class quinoxaline, and the molecular formula is C9H7N3O, Application In Synthesis of 5182-90-1.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Zhu, Haizhou; Mishra, Rosalin; Yuan, Long; Abdul Salam, Safnas F.; Liu, Jing; Gray, George; Sterling, Alyssa D.; Wunderlich, Mark; Landero-Figueroa, Julio; Garrett, Joan T.; Merino, Edward J. published the artcile< Oxidative Cyclization-Induced Activation of a Phosphoinositide 3-Kinase Inhibitor for Enhanced Selectivity of Cancer Chemotherapeutics>, Safety of 7-Nitro-2(1H)-quinoxalinone, the main research area is oxidative cyclization PI3K inhibitor cancer; oxidative cyclization; phosphoinositide 3-kinase inhibitors; prodrugs; reactive oxygen species; synergy effects.

In this work, we designed a prodrug that reacts with cellular oxidative equivalent leading to ether cleavage and cyclization to release an active phosphatidylinositol 3-kinase (PI3K) inhibitor. We show that the compound reduces affinity for PI3KA relative to the PI3K inhibitor, is slow to intercellularly oxidize, and is resistant to liver microsomes. We observed modest activity in untreated acute myeloid leukemia cells and 14-fold selectivity relative to non-cancerous cells. The cellular activity of the compound can be modulated by the addition of antioxidants or oxidants, indicating the compound activity is sensitive to cellular reactive oxygen species (ROS) state. Co-treatment with cytosine arabinoside or doxorubicin was used to activate the compound inside cells. We observed strong synergistic activity specifically in acute myeloid leukemia (AML) cancer cells with an increase in selective anticancer activity of up to 90-fold. Thus, these new self-cyclizing compounds can be used to increase the selectivity of anticancer agents.

ChemMedChem published new progress about Acute myeloid leukemia. 89898-96-4 belongs to class quinoxaline, and the molecular formula is C8H5N3O3, Safety of 7-Nitro-2(1H)-quinoxalinone.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Loriga, Mario; Fiore, Maria; Sanna, Paolo; Paglietti, Giuseppe published the artcile< Quinoxaline chemistry. Part 4. 2-(R)-Anilinoquinoxalines as nonclassical antifolate agents. Synthesis, structure elucidation and evaluation of in vitro anticancer activity>, COA of Formula: C8H4ClN3O2, the main research area is anilinoquinoxaline derivative preparation neoplasm inhibitor; quinoxaline anilino derivative preparation antitumor.

Thirty-five quinoxalines bearing a substituted aniline group on position 2 and various substituents on positions 3,6,7 and 8 were prepared in order to evaluate in vitro anticancer activity. Structural elucidation of some isomeric quinoxalinones formed by ring closure of 4-substituted-1,2-diaminobenzenes with dicarbonyl compounds was achieved by comparison with one isomer coming from an unambiguous independent route. Preliminary in vitro screening at NCI showed that many compounds exhibited a moderate to strong growth inhibition activity on various cells lines between 10-5 and 10-4 molar concentrations

Farmaco published new progress about Antitumor agents. 6272-25-9 belongs to class quinoxaline, and the molecular formula is C8H4ClN3O2, COA of Formula: C8H4ClN3O2.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Nasielski, J.; Heilporn, S.; Nasielski-Hinkens, R.; Tinant, B.; Declercq, J. P. published the artcile< An unexpected ring-opening in the Reissert reaction on 2,3-diphenylquinoxaline N-oxide>, Related Products of 23088-24-6, the main research area is quinoxaline oxide Reissert; phenylquinoxaline oxide Reissert ring cleavage; crystal structure benzaliminobenzoylaniline; mol structure benzaliminobenzoylaniline.

When quinoxaline-N-oxide is reacted with KCN and BzCl in H2O or MeOH; the products are 2-, 5- and 6-chloroquinoxaline and small amounts of 2-cyanoquinoxaline. Using three equivalent of Me3SiCN instead of KCN, and CH2Cl2 as the solvent, leads to a 72% yield of 2-cyanoquinoxaline. The reaction of Me3SiCN and BzCl with 2,3-diphenylquinoxaline-N-oxide leads to 2-Bz2NC6H4N:CPhCN (I). The structure of I is based on spectroscopic data and on an X-ray crystallog. anal.

Tetrahedron published new progress about Crystal structure. 23088-24-6 belongs to class quinoxaline, and the molecular formula is C9H5N3, Related Products of 23088-24-6.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Sangkanu, Suthinee; Rukachaisirikul, Vatcharin; Suriyachadkun, Chanwit; Phongpaichit, Souwalak published the artcile< Evaluation of antibacterial potential of mangrove sediment-derived actinomycetes>, Related Products of 5182-90-1, the main research area is sequence Streptomyces Staphylococcus Acinetobacter Chromobacterium antibacterial violacein; Anti-biofilm; Anti-violacein production; Antibacterial activity; Bioactive metabolites; Mangrove-derived actinomycetes; Streptomyces.

Actinomycetes are well-known as the source of bioactive metabolites. In this work, 16 out of 118 (13.6%) isolates of mangrove sediment-derived actinomycetes showed potential antibacterial activity against at least one bacterial strain. Five extracts from isolates AMA11, AMA12 and AMA21 exhibited a broad spectrum antibacterial activity against Staphylococcus aureus ATCC25923, Staphylococcus epidermidis ATCC35984, methicillin-resistant S. aureus (MRSA) SK1, Acinetobacter baumannii NPRC004 and Escherichia coli ATCC25922. Et acetate extract from the cells of AMA11 (AMA11CE) showed high activity against S. aureus and MRSA with the lowest min. inhibitory concentration (MIC) of 0.5μg ml-1. At concentration of four times its MIC, AMA11CE destroyed MRSA cells as analyzed by the SEM. In addition, AMA11CE, Et acetate extract from the culture broth of AMA12 (AMA12BE), AMA12CE and AMA21CE reduced violacein production in Chromobacterium violaceum. Furthermore, at concentrations lower than 10μg ml-1, all five extracts inhibited biofilm formation by S. epidermidis ATCC35984. The chem. anal. of the most active fraction from AMA11CE by GC-MS revealed the presence of 3-nitro-1,2-benzenedicarboxylic acid, hexadecanoic acid, quinoxaline-2-carboxamide and pentadecanoic acid. The 16S rDNA sequencing anal. revealed that these three potential isolates belonged to the genus Streptomyces. The results revealed that the actinomycetes from mangrove environment would be a good source of bioactive metabolites against pathogenic bacteria.

Microbial Pathogenesis published new progress about Acinetobacter baumannii. 5182-90-1 belongs to class quinoxaline, and the molecular formula is C9H7N3O, Related Products of 5182-90-1.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Gerchakov, Shlomo; Whitman, Peter J.; Schultz, Harry P. published the artcile< Quinoxaline studies. XIII. N-(2-Quinoxaloyl)-α-amino acids>, Synthetic Route of 5182-90-1, the main research area is .

A mixt of α-amino acid, 5% aqueous NaHCO3 and 2-quinoxaloyl chloride was stirred at 25° until the first-formed red color became pale yellow. Acidification of the decolorized solution then yielded the title compounds Uv data are given.

Journal of Medicinal Chemistry published new progress about Amino acids Role: BIOL (Biological Study). 5182-90-1 belongs to class quinoxaline, and the molecular formula is C9H7N3O, Synthetic Route of 5182-90-1.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Sasaki, Yoshio; Hatanaka, Minoru; Suzuki, Miyoko published the artcile< Proton magnetic resonance spectra in aromatic systems. XIII. Heteroaromatic series. 5. 6-Substituted quinoxalines>, Computed Properties of 23088-24-6, the main research area is quinoxalines hetervaroms PMR; hetervaroms quinoxalines PMR; PMR quinoxalines hetervaroms.

The chem. shifts of the ring 1H of 6-quinoxalines have been corrected for N anisotropy, N elec. field, and ring current effects. The corrected shifts have also been correlated with the substituent constants σπ, and those corresponding to the π-electron charge density-ρ-distributions were estimated, and converted to ρ values.

Yakugaku Zasshi published new progress about NMR (nuclear magnetic resonance). 23088-24-6 belongs to class quinoxaline, and the molecular formula is C9H5N3, Computed Properties of 23088-24-6.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Teng, Qing-Hu; Yao, Yan; Wei, Wen-Xiu; Tang, Hai-Tao; Li, Jia-Rong; Pan, Ying-Ming published the artcile< Direct C-H sulfenylation of quinoxalinones with thiols under visible-light-induced photocatalyst-free conditions>, Name: 7-Nitro-2(1H)-quinoxalinone, the main research area is arylthioquinoxalinone alkylthioquinoxalinone preparation; aerobic photochem oxidative sulfenylation quinoxalinone thiol.

Quinoxalinones underwent aerobic photochem. sulfenylation/cross-dehydrogenative coupling with thiols under blue LED irradiation without added photocatalyst in NMP to give aryl- and alkylthioquinoxalinones.

Green Chemistry published new progress about Aromatic thiols Role: RCT (Reactant), RACT (Reactant or Reagent). 89898-96-4 belongs to class quinoxaline, and the molecular formula is C8H5N3O3, Name: 7-Nitro-2(1H)-quinoxalinone.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider

Morokata, Tatsuaki; Suzuki, Keiko; Ida, Kenji; Yamada, Toshimitsu published the artcile< Effect of a novel interleukin-5 receptor antagonist, YM-90709, on antigen-induced eosinophil infiltration into the airway of BDF1 mice>, Recommanded Product: YM-90709, the main research area is YM90709 antiinflammatory IL5 receptor antagonist eosinophil inflammation respiratory tract.

A newly synthesized compound, YM-90709, 2,3-dimethoxy-6,6-dimethyl-5,6-dihydrobenzo[7,8]indolizino[2,3-b]quinoxaline, was previously reported to specifically inhibit the binding of interleukin-5 (IL-5) to its receptor (R) on human eosinophils. In this study, the i.v. injection of YM-90709 inhibited antigen-induced infiltration of eosinophils into the bronchoalveolar lavage fluid (BALF) of BDF1 mice, with an ED50 value of 0.050 mg/kg. Anti-murine IL-5 monoclonal antibody (mAb) also inhibited the infiltration of eosinophils with an ED50 value of 0.035 mg/kg. These results indicate that YM-90709, which is a novel IL-5R antagonist, inhibits antigen-induced eosinophil recruitment into the airway, the same as anti-IL-5 mAb does.

Immunology Letters published new progress about Allergic inflammation. 163769-88-8 belongs to class quinoxaline, and the molecular formula is C22H21N3O2, Recommanded Product: YM-90709.

Referemce:
Quinoxaline – Wikipedia,
Quinoxaline | C8H6N2 | ChemSpider