Heterocyclic Building Blocks-Naphthyridine

Vinoth, M.; Natarajan, B.; Sundaram, C. Shanmuga published the artcile< Characterization and evaluation ethyl acetate extract of melochia corchorifolia leaf-anticancer antibiological and molecular docking studies on breast cancer estrogen receptor>, Reference of 6882-68-4, the main research area is Melochia leaf extract anticancer antibiol breast cancer estrogen receptor.

The present work focused on Phytochem. screening, characterization, anticancer activity and antibiol. activity of Et acetate extract of Melochia corchorifolia leaves followed by mol. docking studies have been carried out. The plant leaves have been collected, weighed, and extracted with the soxhlet apparatus by using Et acetate solvent and then extracted are subjected to phytochem. screening. Antibiol. activity of plant leaves Et acetate extract has been tested against six bacterial and two fungal strains using agar well diffusion methodol. The characterization of phytoconstituents compounds has been carried out using various spectroscopy method such as GC-MS (Gas chromatog. Mass spectroscopy), UV-visible and Fourier-transform IR. Auto dock tool (4.2.0) is used for mol. docking studies. The phytochem. anal. of Melochia corchorifolia Et acetate leaves, reveals the existence of carbohydrates, glycosides, triterpenes flavonoids and alkaloids. Antimicrobial activity is effective against gram-pos. bacterial strains namely Staphylococcus aureus (17 mm), Bacillus subtilis (16 mm), the gram-neg. bacterial strains namely Salmonella typhi (15 mm) and E. coli (14 mm). Moreover, the extract is also found to be effective against Aspergillus Niger (18 mm) fungal species. The GC-MS and FT-IR anal. show bioactive compounds and their functional groups. UV-VIS anal. results reveal that the presence of phytoconstituents derivatives in the range between 206-350 nm. The cytotoxicity activity for the MCF-7 cell line shows that the drug efficacy IC50 value is 148.836 (μg/mL). Further, the predicted bioactive compounds are docked with the cancer estrogen protein receptor (PDB ID: 3s7s) with ligand martidin-15 one shows the highest binding affinity. The study reveals the potential of Melochia corchorifolia leaves Et acetate extract showed antibiol. and anticancer activity.

Indian Journal of Chemical Technology published new progress about Affinity (Binding). 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Reference of 6882-68-4.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Blazejewski, Sara M.; Bennison, Sarah A.; Liu, Xiaonan; Toyo-oka, Kazuhito published the artcile< High-throughput kinase inhibitor screening reveals roles for Aurora and Nuak kinases in neurite initiation and dendritic branching>, Safety of 9-(6-Aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one, the main research area is high throughput screening aurora nuak kinase inhibitor neurite initiation.

Kinases are essential regulators of a variety of cellular signaling processes, including neurite formation-a foundational step in neurodevelopment. Aberrant axonal sprouting and failed regeneration of injured axons are associated with conditions like traumatic injury, neurodegenerative disease, and seizures. Investigating the mechanisms underlying neurite formation will allow for identification of potential therapeutics. We used a kinase inhibitor library to screen 493 kinase inhibitors and observed that 45% impacted neuritogenesis in Neuro2a (N-2a) cells. Based on the screening, we further investigated the roles of Aurora kinases A, B, and C and Nuak kinases 1 and 2. The roles of Aurora and Nuak kinases have not been thoroughly studied in the nervous system. Inhibition or overexpression of Aurora and Nuak kinases in primary cortical neurons resulted in various neuromorphol. defects, with Aurora A regulating neurite initiation, Aurora B and C regulating neurite initiation and elongation, all Aurora kinases regulating arborization, and all Nuak kinases regulating neurite initiation and elongation and arborization. Our high-throughput screening and anal. of Aurora and Nuak kinases revealed their functions and may contribute to the identification of therapeutics.

Scientific Reportspublished new progress about Aurora kinase inhibitors. 1223001-51-1 belongs to class naphthyridine, and the molecular formula is C24H15F3N4O, Safety of 9-(6-Aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Xu, Fei; Li, Xin; Yan, Lili; Yuan, Na; Fang, Yixuan; Cao, Yan; Xu, Li; Zhang, Xiaoying; Xu, Lan; Ge, Chaorong; An, Ni; Jiang, Gaoyue; Xie, Jialing; Zhang, Han; Jiang, Jiayi; Li, Xiaotian; Yao, Lei; Zhang, Suping; Zhou, Daohong; Wang, Jianrong published the artcile< Autophagy promotes the repair of radiation-induced DNA damage in bone marrow hematopoietic cells via enhanced STAT3 signaling>, Electric Literature of 1223001-51-1, the main research area is gamma radiation autophagy DNA damage BM hematopoietic cell.

Autophagy protects hematopoietic cells from radiation damage in part by promoting DNA damage repair. However, the mol. mechanisms by which autophagy regulates DNA damage repair remain largely elusive. Here, we report that this radioprotective effect of autophagy depends on STAT3 signaling in murine bone marrow mononuclear cells (BM-MNCs). Specifically, we found that STAT3 activation and nuclear translocation in BM-MNCs were increased by activation of autophagy with an mTOR inhibitor and decreased by knockout of the autophagy gene Atg7. The autophagic regulation of STAT3 activation is likely mediated by induction of KAP1 degradation, because we showed that KAP1 directly interacted with STAT3 in the cytoplasm and knockdown of KAP1 increased the phosphorylation and nuclear translocation of STAT3. Subsequently, activated STAT3 transcriptionally upregulated the expression of BRCA1, which increased the ability of BM-MNCs to repair radiation-induced DNA damage. This novel finding that activation of autophagy can promote DNA damage repair in BM-MNCs via the ATG-KAP1-STAT3-BRCA1 pathway suggests that autophagy plays an important role in maintaining genomic integrity of BM-MNCs and its activation may confer protection of BM-MNCs against radiationinduced genotoxic stress.

Radiation Researchpublished new progress about Autophagy. 1223001-51-1 belongs to class naphthyridine, and the molecular formula is C24H15F3N4O, Electric Literature of 1223001-51-1.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Ma, Baowei; Athari, Seyyed Shamsadin; Mehrabi Nasab, Entezar; Zhao, Limin published the artcile< PI3K/AKT/mTOR and TLR4/MyD88/NF-κB Signaling Inhibitors Attenuate Pathological Mechanisms of Allergic Asthma>, Computed Properties of 1223001-51-1, the main research area is allergic asthma PI3K AKT mTOR TLR4 MyD88 NFkB; Th; asthma; inflammation; signaling; target therapy; treatment.

Asthma is an inflammatory airway disease wherein bronchoconstriction, airway inflammation, and airway obstruction during asthma attacks are the main problems. It is recognized that imbalance of Th1/Th2 and Th17/Treg is a critical factor in asthma pathogenesis. Manipulation of these with signaling mols. such as mTOR, PI3K, Akt, and MyD88 can control asthma. Mouse model of allergic asthma was produced and treated with ketamine, metformin, metformin and ketamine, triciribine, LY294002, and torin2. MCh challenge test, BALfs Eos Count, the IL-4, 5, INF-γ, eicosanoid, total IgE levels were determined The MUC5a, Foxp3, RORγt, PI3K, mTOR, Akt, PU.1, and MyD88 gene expressions and histopathol. study were done. Asthma groups that were treated with all six components had reduced Penh value, total IgE, IL-4 and IL-5 levels, MUC5a, RORγt, MyD88 and mTOR expression, goblet cell hyperplasia, and mucus hyper-secretion. The eosinophil percentage and Cys-LT level were decreased by metformin and ketamine, triciribine, LY294002, and torin2. The level of IFN-γ was increased in triciribine, LY294002, and torin2. Metformin, metformin and ketamine, triciribine, LY294002, and torin2 reduced Akt and PI3K expression, peribronchial and perivascular inflammation, and increased expression of Foxp3. Torin2 had an effect on PU.1 expression. Inhibition of PI3K/AKT/mTOR and TLR4/MyD88/NF-κB signaling with targeted mols. can attenuate asthma pathol. and play an important role in airways protection.

Inflammationpublished new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (RORgt). 1223001-51-1 belongs to class naphthyridine, and the molecular formula is C24H15F3N4O, Computed Properties of 1223001-51-1.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Zhu, Naiqiang; Hou, Jingyi published the artcile< Molecular mechanism of the anti-inflammatory effects of Sophorae Flavescentis Aiton identified by network pharmacology>, Computed Properties of 6882-68-4, the main research area is Sophora flavescens antiinflammatory effect mol mechanism network pharmacol.

Inflammation, a protective response against infection and injury, involves a variety of biol. processes. Sophorae Flavescentis (Kushen) is a promising Traditional Chinese Medicine (TCM) for treating inflammation, but the pharmacol. mechanism of Kushen’s anti-inflammatory effect has not been fully elucidated. The bioactive compounds, predicted targets, and inflammation-related targets of Kushen were obtained from open source databases. The ”Component-Target” network and protein-protein interaction (PPI) network were constructed, and hub genes were screened out by topol. anal. Gene ontol. (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) enrichment analyses were performed on genes in the PPI network. Furthermore, nitric oxide (NO) production anal., RT-PCR, and western blot were performed to detect the mRNA and protein expression of hub genes in LPS-induced RAW264.7 cells. An immunofluorescence assay found that NF-κB p65 is translocated. A total of 24 bioactive compounds, 465 predicted targets, and 433 inflammation-related targets were identified and used to construct ”Component-Targets” and PPI networks. Then, the five hub genes with the highest values-IL-6, IL-1β, VEGFA, TNF-α, and PTGS2 (COX-2)- were screened out. Enrichment anal. results suggested mainly involved in the NF-κB signaling pathway. Moreover, experiments were performed to verify the predicted results. Kushen may mediate inflammation mainly through the IL-6, IL-1β, VEGFA, TNF-α, and PTGS2 (COX-2), and the NF-κB signaling pathways. This finding will provide clin. guidance for further research on the use of Kushen to treat inflammation.

Scientific Reportspublished new progress about Anti-inflammatory agents. 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Computed Properties of 6882-68-4.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Ponsford, Amy H.; Ryan, Thomas A.; Raimondi, Andrea; Cocucci, Emanuele; Wycislo, Susanne A.; Frohlich, Florian; Swan, Laura E.; Stagi, Massimiliano published the artcile< Live imaging of intra-lysosome pH in cell lines and primary neuronal culture using a novel genetically encoded biosensor>, Related Products of 1223001-51-1, the main research area is chloroquine fluorescence microscopy lysosome MTOR protein pH Vtype ATPase; Chloroquine; MTOR protein; V-type ATPase; fluorescence microscopy; lysosomes; pH.

Disorders of lysosomal physiol. have increasingly been found to underlie the pathol. of a rapidly growing cast of neurodevelopmental disorders and sporadic diseases of aging. One cardinal aspect of lysosomal (dys)function is lysosomal acidification in which defects trigger lysosomal stress signaling and defects in proteolytic capacity. We have developed a genetically encoded ratiometric probe to measure lysosomal pH coupled with a purification tag to efficiently purify lysosomes for both proteomic and in vitro evaluation of their function. Using our probe, we showed that lysosomal pH is remarkably stable over a period of days in a variety of cell types. Addnl., this probe can be used to determine that lysosomal stress signaling via TFEB is uncoupled from gross changes in lysosomal pH. Finally, we demonstrated that while overexpression of ARL8B GTPase causes striking alkalinization of peripheral lysosomes in HEK293 T cells, peripheral lysosomes per se are no less acidic than juxtanuclear lysosomes in our cell lines.

Autophagypublished new progress about Acidification. 1223001-51-1 belongs to class naphthyridine, and the molecular formula is C24H15F3N4O, Related Products of 1223001-51-1.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Dai, Lin-Lin; Li, Dong-Dong; Zhao, Xiu-Mei; Zhi, Shuang; Shen, Hong-Sheng; Yang, Zi-Bo published the artcile< Synthesis and Antitumor Effect of Sophoridine Derivatives Bearing an Acyclic Aryloxy Phosphoramidate Mustard Functionality>, Computed Properties of 6882-68-4, the main research area is sophoridine aryloxy phosphoramidate mustard synthesis antitumor.

To elevate the potency of sophoridine, phosphoramidate mustard motif was incorporated to D-ring opened sophoridine scaffold. A series of acyclic aryloxy phosphoramidate mustard functionalized sophoridine derivatives were synthesized and screened for cytostatic activity in a range of different tumor cell lines (S180, H22, K562, MCF-7, SMMC-7721, and LoVo). All these compounds were shown to be more sensitive to S180 and H22 cells with IC50 values ranging from 2.10 to 7.21 μM. In addition, all targeted derivatives distinctly are more cytotoxic to cancer cells than normal cell L929. Compounds I (R = 3-ClC6H4, 4-BrC6H4, 1-naphthyl, 2-naphthyl) displayed moderate tumor suppression without apparent organ toxicity in vivo against mice bearing H22 liver tumors. Their potential binding modes with DNA topoisomerase I complex have also been investigated.

Journal of Heterocyclic Chemistrypublished new progress about Antitumor agents. 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Computed Properties of 6882-68-4.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Feehan, Robert P.; Nelson, Amanda M.; Shantz, Lisa M. published the artcile< Inhibition of mTORC2 enhances UVB-induced apoptosis in keratinocytes through a mechanism dependent on the FOXO3a transcriptional target NOXA but independent of TRAIL>, Product Details of C24H15F3N4O, the main research area is mTORC UVB keratinocyte apoptosis FOXOa transcription NOXA TRAIL; Apoptosis; NOXA; Non-melanoma skin cancer; TRAIL; UVB; mTOR.

The primary cause of non-melanoma skin cancer (NMSC) is UV B (UVB) radiation. We have shown previously that mTORC2 inhibition sensitizes keratinocytes to UVB-induced apoptosis mediated by the transcription factor FOXO3a. FOXO3a is a key regulator of apoptosis and a tumor suppressor in several cancer types. Activation of FOXO3a promotes apoptosis through the coordinated expression of a variety of target genes, including TRAIL and NOXA. We hypothesized that in the setting of mTORC2 inhibition, the UVB-induced expression of these factors would lead to apoptosis in a FOXO3a-dependent manner. Using spontaneously immortalized human keratinocytes (HaCaT cells), we observed that both TRAIL and NOXA expression increased in cells exposed to UVB and the TOR kinase inhibitor Torin 2. Similar to knockdown of FOXO3a, NOXA knockdown reversed the sensitization to UVB-induced apoptosis caused by mTORC2 inhibition. In contrast, loss of TRAIL by either knockdown or knockout actually enhanced expression of nuclear FOXO3a, which maintained apoptosis. These surprising results are not due to faulty death receptor signaling in HaCaT cells, as we found that the cells undergo extrinsic apoptosis in response to treatment with recombinant TRAIL. Even more striking, TRAIL knockout cells were sensitized to recombinant TRAIL-induced apoptosis compared to wild-type HaCaT cells, with the largest increase occurring in the presence of mTORC2 inhibition. Taken together, these studies provide strong evidence that mTORC2 controls UVB-induced apoptosis by regulating NOXA expression downstream of FOXO3a. Moreover, FOXO3a transcriptional activation by mTORC2 inhibitors may be a valuable target for prevention or therapy of NMSC, especially in cases with low endogenous TRAIL.

Cellular Signallingpublished new progress about Animal gene Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (NOXA). 1223001-51-1 belongs to class naphthyridine, and the molecular formula is C24H15F3N4O, Product Details of C24H15F3N4O.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Hamed, Mohamed; Gladbach, Yvonne; Moeller, Steffen; Fischer, Sarah; Ernst, Mathias; Struckmann, Stephan; Storch, Alexander; Fuellen, Georg published the artcile< A workflow for the integrative transcriptomic description of molecular pathology and the suggestion of normalizing compounds, exemplified by Parkinson's disease>, Related Products of 1223001-51-1, the main research area is miRNA mRNA Parkinson disease mol pathol.

The volume of mol. observations on human diseases in public databases is continuously increasing at accelerating rates. A bottleneck is their computational integration into a coherent description, from which researchers may derive new well-founded hypotheses. Also, the need to integrate data from different technologies (genetics, coding and regulatory RNA, proteomics) emerged in order to identify biomarkers for early diagnosis and prognosis of complex diseases and therefore facilitating the development of novel treatment approaches. We propose here a workflow for the integrative transcriptomic description of the mol. pathol. in Parkinsons’s Disease (PD), including suggestions of compounds normalizing disease-induced transcriptional changes as a paradigmatic example. We integrated gene expression profiles, miRNA signatures, and publicly available regulatory databases to specify a partial model of the mol. pathophysiol. of PD. Six genetic driver elements (2 genes and 4 miRNAs) and several functional network modules that are associated with PD were identified. Functional modules were assessed for their statistical significance, cellular functional homogeneity, literature evidence, and normalizing small mols. In summary, our workflow for the joint regulatory anal. of coding and non-coding RNA, has the potential to yield clin. as well as biol. relevant information, as demonstrated here on PD data.

Scientific Reportspublished new progress about Auxilin 1 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 1223001-51-1 belongs to class naphthyridine, and the molecular formula is C24H15F3N4O, Related Products of 1223001-51-1.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem

Huo, Zhixia; Chen, Lei published the artcile< Base-deactivated and alkaline-resistant chromatographic stationary phase based on functionalized polymethylsilsesquioxane microspheres>, Electric Literature of 6882-68-4, the main research area is base deactivated chromatog stationary phase functionalized polymethylsilsesquioxane microsphere; basic compounds; co-condensation; functionalization; polymethylsilsesquioxane; silanol activity.

Vinyl, chloropropyl, and mercaptopropyl functionalized particles were prepared by a two-step acidic/alk. catalyzed co-hydrolysis/condensation of methyltrimethoxysilane with a different silane precursor that carries chem. reactive functional group including vinyl, chloropropyl, and mercaptopropyl, resp. The morphol., pore structure, and functional groups of the synthesized packings were studied by SEM, nitrogen adsorption-desorption measurements, and solid-state 13C 29Si NMR spectroscopy, resp. The particles show ordered sphere, narrow particle size distribution, and mesoporous structure. The carbon contents of the microspheres are in the range of 17-19%, comparable to those of octadecyl-bonded silica packings. The three-kind of microspheres were directly used as packing materials for high-performance liquid chromatog. without size classification. The chromatog. performance of the columns was evaluated and compared with a com. available C18 phase. The results revealed that these columns possess typical reversed-phase chromatog. properties with increased hydrophobicity than polymethylsilsesquioxane and sym. peaks for basic compounds They were applied to the simultaneous separation of combination bendazol hydrochlorothiazide capsules containing polar and basic drugs with peaks identified by tandem with mass spectrometry. In general, a novel method is provided for the synthesis of different methyltrimethoxysilane-derived microspheres for high-performance liquid chromatog., which are advantageous for separating basic compounds

Journal of Separation Sciencepublished new progress about Chromatographic stationary phases (base-deactivated and alk.-resistant). 6882-68-4 belongs to class naphthyridine, and the molecular formula is C15H24N2O, Electric Literature of 6882-68-4.

Referemce:
1,8-Naphthyridine – Wikipedia,
1,8-Naphthyridine | C8H6N2 – PubChem