Category: naphthyridine

Raj, Mamta published the artcileGraphene/conducting polymer nano-composite loaded screen printed carbon sensor for simultaneous determination of dopamine and 5-hydroxytryptamine, Name: 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, the publication is Sensors and Actuators, B: Chemical (2017), 993-1002, database is CAplus.

A novel and sensitive electrochem. method has been developed for the simultaneous determination of dopamine (DA) and 5-hydroxytryptamine (5-HT) using graphene (GR) and poly 4-amino-3-hydroxy-1-naphthalenesulfonic acid modified screen printed carbon sensor. The electrochem. measurements were studied using cyclic voltammetry, square wave voltammetry, whereas the surface morphol. of the modified sensor was characterized by Electrochem. Impedance Spectroscopy and Field Emission SEM. The fabricated sensor facilitated the anal. of DA and 5-HT in the concentration range 0.05-100μM and 0.05-150μM with the detection limit of 2 nM and 3 nM resp. The fabricated sensor has been explored for the determination of 5-HT in the plasma samples and the selectivity of the proposed work has been proved by the anal. of DA and 5-HT in the presence of common metabolites present in biol. fluids. The anal. applicability of the fabricated sensor has also been successfully demonstrated for the simultaneous detection of DA and 5-HT in the pharmacol. formulations, human urine and blood samples.

Sensors and Actuators, B: Chemical published new progress about 116-63-2. 116-63-2 belongs to naphthyridine, auxiliary class Sulfonic acid,Amine,Naphthalene,Alcohol,Organic Pigment, name is 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, and the molecular formula is C10H9NO4S, Name: 4-Amino-3-hydroxynaphthalene-1-sulfonic acid.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Witta, Samir E. published the artcileA phase I and pharmacokinetic study of exisulind and docetaxel in patients with advanced solid tumors, SDS of cas: 59973-80-7, the publication is Clinical Cancer Research (2004), 10(21), 7229-7237, database is CAplus and MEDLINE.

Exisulind (sulindac sulfone, FGN-1, Aptosyn) is a sulindac metabolite that induces apoptosis via inhibition of cyclic GMP-phosphodiesterase. This agent demonstrated tumor growth inhibition in rodent models of colon, breast, prostate, and lung carcinogenesis. In an orthotopic model of human non-small-cell lung cancer, the combination of exisulind and docetaxel prolonged survival in athymic nude rats, forming the basis of this phase I combination study. This study evaluated the toxicity and pharmacokinetics of combining exisulind (150-250 mg) given orally twice daily and docetaxel (30-36 mg/m²) administered i.v. on days 1, 8, and 15 of a 4-wk cycle. Twenty patients with a range of advanced solid tumors (median age, 59 years; age range, 35-77 years; median performance status, 1) received a total of 70 courses. Observed adverse events were mild to moderate, and there was no dose-limiting toxicity at any level. Grade 3 gastrointestinal toxicities were present in 10 of the 70 cycles (10%) and included nausea, vomiting, dyspepsia, and elevated alk. phosphatase. Neutropenia was present in four cycles in patients treated with a docetaxel dose of 36 mg/m². Pharmacokinetic anal. did not demonstrate a clear effect of exisulind on docetaxel pharmacokinetics and vice versa. Relationships were evident between the plasma concentration of exisulind and the development of grade 2 or greater toxicities. One third of patients maintained stable disease for 3 to 12 cycles, but no objective responses were observed The combination of docetaxel (36 mg/m², weekly) and exisulind (500 mg/d) was reasonably well tolerated, and it is undergoing phase II testing in patients with non-small-cell lung cancer.

Clinical Cancer Research published new progress about 59973-80-7. 59973-80-7 belongs to naphthyridine, auxiliary class Immunology/Inflammation,COX, name is Sulindac sulfone, and the molecular formula is C19H17N2NaO4S, SDS of cas: 59973-80-7.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Dawson, Nancy A. published the artcileA phase II study of estramustine, docetaxel, and exisulind in patients with hormone-refractory prostate cancer: results of cancer and leukemia group B trial 90004, Related Products of naphthyridine, the publication is Clinical Genitourinary Cancer (2008), 6(2), 110-116, database is CAplus and MEDLINE.

Docetaxel/estramustine is a known active regimen in hormone-refractory prostate cancer (HRPC). A phase II study was conducted to assess the safety and efficacy of docetaxel/estramustine combined with exisulind, an apoptotic antineoplastic drug. Eighty men with chemotherapy-naive HRPC were enrolled in a multicenter, cooperative group study. The treatment regimen consisted of oral estramustine (280 mg 3 times daily for 5 days), docetaxel 70 mg/m², oral exisulind (250 mg twice daily), oral dexamethasone (8 mg twice daily for 3 days), and oral warfarin (2 mg daily). Seventy-five eligible patients were treated with a median of 6 cycles of therapy. Forty-seven patients (62.7%; 95% CI, 50.7-73.6%) had a â‰?50% decline in prostate-specific antigen levels. Forty-six patients had measurable disease with 6 partial responses (13%; 95% CI, 4.9-26.3%). The main grade 3/4 toxicities were neutrophils (79%), fatigue (15%), and thrombosis/embolism (10%). The median time to first progression was 5.1 mo (95% CI, 4.4-6.3 mo) and the median survival time was 17.8 mo (95% CI, 14.7-20.1 mo). The combination of estramustine/docetaxel/exisulind was associated with significant thomboembolic toxicity despite prophylactic warfarin. The contribution of exisulind to toxicity is uncertain. Prostate-specific antigen decline, response rates, and progression-free and overall survival are similar to those reported with docetaxel/estramustine.

Clinical Genitourinary Cancer published new progress about 59973-80-7. 59973-80-7 belongs to naphthyridine, auxiliary class Immunology/Inflammation,COX, name is Sulindac sulfone, and the molecular formula is C20H17FO4S, Related Products of naphthyridine.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Sun, Lilin published the artcileIndication of critical micelle concentration of nonionic surfactants with large emission change using water-soluble conjugated polymer as molecular light switch, Quality Control of 18512-55-5, the publication is Journal of Luminescence (2013), 260-265, database is CAplus.

A new near-IR water-soluble conjugated polymer, i.e. poly [2,5-di (propyloxysulfonate)-1,4-phenylene-ethynylene-9,10-anthrylene] (PPEASO3) was synthesized to investigate its interaction with surfactants. It was found that PPEASO3 has only a weak fluorescence emission at about 670 nm due to its self-aggregation in water and in aqueous solution containing a low concentration of nonionic surfactants, i.e. below their critical micelle concentration (CMC). However, a dramatic fluorescence enhancement with a large emission blue-shift (>40 nm) was found once the concentration of nonionic surfactants reached the CMC (especially for Triton X-100). An orange fluorescence could be observed even with naked-eyes under UV-lamp, which gave a direct indication for the micelle forming process and provided a simple method for the CMC determination of the nonionic surfactants. The CMC values determined by this method were in good agreement with those obtained by other techniques. The dramatic emission change observed could be ascribed to the intensive hydrophobic interaction between PPEASO3 and surfactants micelle, which greatly disrupts the aggregation of the polymer and increase the fluorescence efficiency of PPEASO3.

Journal of Luminescence published new progress about 18512-55-5. 18512-55-5 belongs to naphthyridine, auxiliary class Alkynyl,Anthracene, name is 9,10-Diethynylanthracene, and the molecular formula is C21H24O8, Quality Control of 18512-55-5.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Shishimi, Toru published the artcileBrF₃-KHF₂: An air-stable fluorinating reagent, Related Products of naphthyridine, the publication is Journal of Fluorine Chemistry (2014), 55-60, database is CAplus.

BrF₃-KHF₂, an air-stable solid prepared from BrF₃ and KHF₂, was used in the various fluorination reactions, including desulfurizing fluorination reactions of benzylic sulfides, ketone and aldehyde dithioacetals, (phenylthio)glycosides, and tri-Me trithioorthocarboxylates. As the results, one to three fluorine atoms were selectively introduced to the substrates.

Journal of Fluorine Chemistry published new progress about 53731-26-3. 53731-26-3 belongs to naphthyridine, auxiliary class Difluoromethyl,Fluoride,Naphthalene, name is 1-(Difluoromethyl)naphthalene, and the molecular formula is C6H12N2O, Related Products of naphthyridine.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Dhamodharan, V. published the artcileSelective G-quadruplex DNA Stabilizing Agents Based on Bisquinolinium and Bispyridinium Derivatives of 1,8-Naphthyridine, Product Details of C10H10N2, the publication is Journal of Organic Chemistry (2012), 77(1), 229-242, database is CAplus and MEDLINE.

Various biol. relevant G-quadruplex DNA structures offer a platform for therapeutic intervention for altering the gene expression or by halting the function of proteins associated with telomeres. One of the prominent strategies to explore the therapeutic potential of quadruplex DNA structures is by stabilizing them with small mol. ligands. Here the synthesis of bisquinolinium and bispyridinium derivatives of 1,8-naphthyridine, e.g., I, and their interaction with human telomeric DNA and promoter G-quadruplex forming DNAs, is reported. The interactions of ligands with quadruplex forming DNAs were studied by various biophys., biochem., and computational methods. Results indicated that bisquinolinium ligands bind tightly and selectively to quadruplex DNAs at low ligand concentration (âˆ?.2-0.4 μM). Furthermore, thermal melting studies revealed that ligands imparted higher stabilization for quadruplex DNA (an increase in the T_m of up to 21 °C for human telomeric G-quadruplex DNA and >25 °C for promoter G-quadruplex DNAs) than duplex DNA (ΔT_m â‰?1.6 °C). Mol. dynamics simulations revealed that the end-stacking binding mode was favored for ligands with low binding free energy. Taken together, the results indicate that the naphthyridine-based ligands with quinolinium and pyridinium side chains form a promising class of quadruplex DNA stabilizing agents having high selectivity for quadruplex DNA structures over duplex DNA structures.

Journal of Organic Chemistry published new progress about 14903-78-7. 14903-78-7 belongs to naphthyridine, auxiliary class 6.6_Aromatics,Naphthyridines, name is 2,7-Dimethyl-1,8-naphthyridine, and the molecular formula is C10H10N2, Product Details of C10H10N2.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Gardner, S. H. published the artcileEffect of nonsteroidal anti-inflammatory drugs on β-catenin protein levels and catenin-related transcription in human colorectal cancer cells, Recommanded Product: Sulindac sulfone, the publication is British Journal of Cancer (2004), 91(1), 153-163, database is CAplus and MEDLINE.

Elevated β-catenin levels in human colorectal cancer (CRC) cells lead to increased trans-activation of ‘protumorigenic’ β-catenin/T-cell factor (TCF) target genes such as cyclin D1. Therefore, possible targets for the anti-CRC activity of nonsteroidal anti-inflammatory drugs (NSAIDs) are β-catenin and catenin-related transcription (CRT). We tested the antiproliferative activity and the effects on levels of β-catenin and cyclin D1 protein, as well as CRT (measured using a synthetic β-catenin/TCF-reporter gene [TOPflash]), of a panel of NSAIDs (indomethacin, diclofenac, sulindac sulfide and sulfone, rofecoxib; range 10-600 μM) on SW480 human CRC cells in vitro. Following NSAID treatment, there was no consistent relation between reduced cell proliferation, induction of apoptosis and changes in β-catenin protein levels or CRT. All the NSAIDs, except rofecoxib, decreased nuclear β-catenin content and cyclin D1 protein levels in parallel with their antiproliferative activity. However, cyclin D1 down-regulation occurred prior to a decrease in total β-catenin protein levels and there was no correlation with changes in CRT, suggesting the existence of CRT-independent effects of NSAIDs on cyclin D1 expression. In summary, NSAIDs have differential effects on β-catenin protein and CRT, which are unlikely to fully explain their effects on cyclin D1 and their antiproliferative activity on human CRC cells in vitro.

British Journal of Cancer published new progress about 59973-80-7. 59973-80-7 belongs to naphthyridine, auxiliary class Immunology/Inflammation,COX, name is Sulindac sulfone, and the molecular formula is C20H17FO4S, Recommanded Product: Sulindac sulfone.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Takahashi, Ikko published the artcileBronsted acid-catalyzed tandem cycloaromatization of naphthalene-based bisacetals: selective synthesis of ortho-fused six-hexagon benzenoids, Quality Control of 152873-79-5, the publication is Chemistry Letters (2017), 46(3), 392-394, database is CAplus.

Naphthalenes bearing two acetal moieties connected by a methylene-2,1-phenylene group underwent regioselective tandem cycloaromatization using a catalytic amount of trifluoromethanesulfonic acid in 1,1,1,3,3,3-hexafluoropropan-2-ol. Five substrates were successfully employed in this protocol to afford ortho-fused six-hexagon benzenoids with high selectivities and in excellent yields.

Chemistry Letters published new progress about 152873-79-5. 152873-79-5 belongs to naphthyridine, auxiliary class Trifluoromethyl,Sulfonate,Benzene, name is 1,5-NAphthalenebis(trifluoromethanesulfonate), and the molecular formula is C12H9NO, Quality Control of 152873-79-5.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Faroughi Niya, Homayoun published the artcileSynthesis, characterization, and application of CoFe₂O₄@amino-2-naphthol-4-sulfonic acid as a novel and reusable catalyst for the synthesis of spirochromene derivatives, HPLC of Formula: 116-63-2, the publication is Applied Organometallic Chemistry (2021), 35(3), e6119, database is CAplus.

In the present work, 1-amino-2-naphthol-4-sulfonic acid immobilized on functionalized CoFe₂O₄ nanoparticles was successfully synthesized as a new, efficient, and recoverable catalyst and tested for the synthesis of spirochromene derivatives by a simple, green, and inexpensive procedure [e.g., isatin + malononitrile + dimedone â†?I (95%)]. This magnetically heterogeneous nanocatalyst was characterized by various techniques such as Fourier transform IR (FT-IR), thermal gravimetric anal. (TGA)/derivative thermogravimetric (DTG), X-ray diffraction (XRD), X-ray mapping, transmission electron microscopy (TEM), energy-dispersive X-ray spectroscopy (EDS), vibrating sample magnetometer (VSM), Brunauer-Emmett-Teller (BET), and SEM analyses. The novel synthesized nanocatalyst can be easily separated and can also be reused several times without appreciable loss in its catalytic activity. Furthermore, in comparison with previous reports, this nanocatalyst showed high thermal stability and acidic properties.

Applied Organometallic Chemistry published new progress about 116-63-2. 116-63-2 belongs to naphthyridine, auxiliary class Sulfonic acid,Amine,Naphthalene,Alcohol,Organic Pigment, name is 4-Amino-3-hydroxynaphthalene-1-sulfonic acid, and the molecular formula is C10H9NO4S, HPLC of Formula: 116-63-2.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem

Mahapatra, Ajit K. published the artcileA highly sensitive and selective ratiometric fluorescent probe based on conjugated donor-acceptor-donor constitution of 1,8-naphthyridine for Hg²⁺, Computed Properties of 14903-78-7, the publication is Journal of Photochemistry and Photobiology, A: Chemistry (2011), 222(1), 47-51, database is CAplus.

A new 1,8-naphthyridine based di-olefinic chemosensor was designed, synthesized and its sensing behavior towards metal ions was investigated by UV-vis, fluorescence and ¹H NMR spectroscopic methods. A highly Hg²⁺-selective fluorescence enhancing property (>1.5-fold) in conjunction with a visible colorimetric change from yellow to purple has been observed, leading to a potential fabrication of both “naked-eye” and fluorescence detection of Hg²⁺. Our designed sensor of the donor-acceptor-donor system shows high selectivity towards mercury(II) ion over other competing metal ions.

Journal of Photochemistry and Photobiology, A: Chemistry published new progress about 14903-78-7. 14903-78-7 belongs to naphthyridine, auxiliary class 6.6_Aromatics,Naphthyridines, name is 2,7-Dimethyl-1,8-naphthyridine, and the molecular formula is C10H10N2, Computed Properties of 14903-78-7.

Referemce:
https://en.wikipedia.org/wiki/1,8-Naphthyridine,
1,8-Naphthyridine | C8H6N2 – PubChem