Month: December 2022

Song, Zhiyong published the artcileDegradation and detoxification of azo dyes by a salt-tolerant yeast Cyberlindnera samutprakarnensis S4 under high-salt conditions, Related Products of naphthyridine, the publication is World Journal of Microbiology & Biotechnology (2018), 34(9), 1-13, database is CAplus and MEDLINE.

A new yeast strain which was capable of degrading various azo dyes under high-salt conditions was identified in this study. The results showed that the yeast named S4 was identified as Cyberlindnera samutprakarnensis through 26S rDNA sequence anal. and could decolorize more than 97% of Acid Red B (ARB) within 18 h under the optimal conditions. The acute toxicity of ARB sharply decreased after degradation NADH-DCIP reductase and lignin peroxidase were determined as the key reductase and oxidase of the yeast S4, resp. Furthermore, it was proposed that ARB was degraded by strain S4 successively through reduction of azo bonds, hydroxylation, deamination, desulfonation and finally to the TCA cycle.

World Journal of Microbiology & Biotechnology 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 C10H19NO3, Related Products of naphthyridine.

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

Elwich-Flis, S. published the artcileAnti-Angiogenic and Apoptotic Effects of Metabolites of Sulindac on Chick Embryo Chorioallantoic Membrane, Related Products of naphthyridine, the publication is Hybridoma and Hybridomics (2003), 22(1), 55-60, database is CAplus and MEDLINE.

Sulindac and other nonsteroidal anti-inflammatory drugs (NSAIDs), in addition to anti-inflammatory properties, express preventive activity against colon cancer. This antineoplastic effect may result from the suppression of polyp development in patients with familial adenomatous polyposis. However, despite intense investigations the exact mechanism for sulindac protective effect is not fully elucidated. Angiogenesis, the process of new blood vessel formation, is required to support tumor growth and may be partially involved in the transformation of polyps into tumor. Therefore, we tested the hypothesis whether sulindac might inhibit angiogenesis. The effects of sulindac metabolites, sulindac sulfide and sulindac sulfone, on vascular development were evaluated using the chick embryo chorioallantoic membrane (CAM) assay in vivo. The angiogenic response was quantitated by several methods including direct stereomicroscopic observation, measurements of Hb content and DNA synthesis whereas quantitation of apoptosis was based on determinations of caspase-3 activity, caspase-3 and bax protein expression, and nuclear DNA fragmentation. Our results indicated that both sulindac metabolites were equally effective in inhibition of new blood vessel formation in CAM during chick embryo development. Moreover, both metabolites of sulindac induced apoptosis in parallel with inhibition of angiogenesis.

Hybridoma and Hybridomics 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

Kotha, Sambasivarao published the artcileModular Approach to Benzofurans, 2H-Chromenes and Benzoxepines via Claisen Rearrangement and Ring-Closing Metathesis: Access to Phenylpropanoids, Computed Properties of 159-62-6, the publication is Chemistry – An Asian Journal (2022), 17(8), e202200084, database is CAplus and MEDLINE.

Benzofurans, 2H-chromenes and benzoxepines are key structural elements present in several natural products and pharmaceuticals. Here, an easy-to-execute strategy for the synthesis of benzofurans, 2H-chromenes and benzoxepines, by employing Claisen rearrangement and ring-closing metathesis as key steps is reported. A variety of phenols were converted into useful oxacycles in good to excellent yields. The ring-closing metathesis approach has been used to produce phenylpropanoid natural products. Examples described here include, the naturally occurring benzofurans such as 7-methoxywutaifuranal, 7-methoxywutaifuranol, 7-methoxywutaifuranate and the O-prenylated natural products like boropinic acid, boropinols A and C.

Chemistry – An Asian Journal published new progress about 159-62-6. 159-62-6 belongs to naphthyridine, auxiliary class Other Aromatic Heterocyclic,Spiro, name is Spiro[fluorene-9,9′-xanthene], and the molecular formula is C25H16O, Computed Properties of 159-62-6.

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

Deguchi, Atsuko published the artcileVasodilator-stimulated phosphoprotein (VASP) phosphorylation provides a biomarker for the action of exisulind and related agents that activate protein kinase G, Application In Synthesis of 59973-80-7, the publication is Molecular Cancer Therapeutics (2002), 1(10), 803-809, database is CAplus and MEDLINE.

Recent studies provide evidence that exisulind and two potent derivatives, CP461 and CP248, induce apoptosis in colon cancer cells by inhibiting cGMP-specific phosphodiesterases (phosphodiesterases 2 and 5). This causes an increase in intracellular levels of cGMP, thus activating the cGMP-dependent protein kinase G (PKG), which then activates pathways that lead to apoptosis. To further examine this mechanism and to provide a potential in vivo biomarker for activation of this pathway, we examined phosphorylation of the vasodilator-stimulated phosphoprotein (VASP), a ubiquitously expressed endogenous substrate for PKG. We found that VASP was phosphorylated after treating SW480 colon cancer cells with exisulind, CP461, or CP248. CP248-induced VASP phosphorylation was inhibited by a specific PKG inhibitor but not by a protein kinase A inhibitor. The drug 3-(5′-hydroxymethyl-2′-furyl)benzylindazole and nitric oxide donors that activate cellular guanylyl cyclase and thus increase cellular levels of cGMP also caused VASP phosphorylation. With all of these agents, the phosphorylation of VASP was associated with increased intracellular levels of cGMP and the induction of apoptosis. We also demonstrated direct in vivo phosphorylation of VASP with constitutively activated mutants of PKG. These results suggest that VASP phosphorylation can provide a useful endogenous cellular biomarker for anticancer agents that cause cGMP-mediated apoptosis.

Molecular Cancer Therapeutics 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, Application In Synthesis of 59973-80-7.

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

Majumdar, Moumita published the artcileMapping the Transformation [{Ru^II(CO)₃Cl₂}₂] to [Ru^I₂(CO)₄]²⁺: Implications in Binuclear Water-Gas Shift Chemistry, Name: 2,7-Dimethyl-1,8-naphthyridine, the publication is Chemistry – A European Journal (2010), 16(8), 2574-2585, S2574/1-S2574/12, database is CAplus and MEDLINE.

The complete sequence of reactions in the base-promoted reduction of [{Ru^II(CO)₃Cl₂}₂] to [Ru^I₂(CO)₄]²⁺ has been unraveled. Several μ-OH, μ:κ²-CO₂H-bridged diruthenium(II) complexes have been synthesized; they are the direct results of the nucleophilic activation of metal-coordinated carbonyls by hydroxides. The isolated compounds are [Ru₂(CO)₄(μ:κ²-C,O-CO₂H)₂(μ-OH)(NP^F-Am)₂][PF₆] (1; NP^F-Am=2-amino-5,7-trifluoromethyl-1,8-naphthyridine) and [Ru₂(CO)₄(μ:κ²-C,O-CO₂H)(μ-OH)(NP-Me₂)₂][BF₄]₂ (2), secured by the applications of naphthyridine derivatives In the absence of any capping ligand, a tetranuclear complex [Ru₄(CO)₈(H₂O)₂(μ³-OH)₂(μ:κ²-C,O-CO₂H)₄][CF₃SO₃]₂ (3) is isolated. The bridging hydroxido ligand in 1 is readily replaced by a π-donor chlorido ligand, which results in [Ru₂(CO)₄(μ:κ²-C,O-CO₂H)₂(μ-Cl)(NP-PhOMe)₂][BF₄] (4). The production of [Ru₂(CO)₄]²⁺ has been attributed to the thermally induced decarboxylation of a bis(hydroxycarbonyl)-diruthenium(II) complex to a dihydrido-diruthenium(II) species, followed by dinuclear reductive elimination of mol. hydrogen with the concomitant formation of the Ru^I-Ru^I single bond. This work was originally instituted to find a reliable synthetic protocol for the [Ru₂(CO)₄(CH₃CN)₆]²⁺ precursor. It is herein prescribed that at least four equivalent of base, complete removal of chlorido ligands by Tl^I salts, and heating at reflux in acetonitrile for a period of four hours are the conditions for the optimal conversion. Premature quenching of the reaction resulted in the isolation of a trinuclear Ru^I₂Ru^II complex [{Ru(NP-Am)₂(CO)}{Ru₂(NP-Am)₂(CO)₂(μ-CO)₂}(μ₃:κ³-C,O,O’-CO₂)][BF₄]₂ (6). These unprecedented diruthenium compounds are the dinuclear congeners of the water-gas shift (WGS) intermediates. The possibility of a dinuclear pathway eliminates the inherent contradiction of pH demands in the WGS catalytic cycle in an alk. medium. A cooperative binuclear elimination could be a viable route for hydrogen production in WGS chem.

Chemistry – A European Journal 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, Name: 2,7-Dimethyl-1,8-naphthyridine.

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

Ghatak, Tapas published the artcileA bicarbonate bridged diruthenium(I) complex: Key evidence for the decarboxylation step in the base-assisted reduction of Ru₂Cl₄(CO)₆, Product Details of C10H10N2, the publication is Inorganica Chimica Acta (2011), 372(1), 94-99, database is CAplus.

Base-assisted reduction of [Ru(CO)₃Cl₂]₂ in the presence of NP-Me₂ (2,7-dimethyl-1,8-naphthyridine) in THF provides an unsupported diruthenium(I) complex [Ru₂(CO)₄Cl₂(NP-Me₂)₂] (1). Two NP-Me₂ and four carbonyls bind at equatorial positions and two chlorides occupy sites trans to the Ru-Ru single bond. Reaction of [Ru(CO)₃Cl₂]₂, TlOTf, KOH and NP-Me₂ in MeCN, in a sealed container, affords a bicarbonate bridged diruthenium(I) complex [Ru₂(CO)₂(μ-CO)₂(μ-O₂COH)(NP-Me₂)₂](OTf) (2). The in situ generated CO₂ is the source for bicarbonate under basic reaction medium. Isolation of 2 validates the decarboxylation step in the base-assisted reduction of [Ru^II(CO)₃Cl₂]₂ → [Ru^I₂(CO)₄]²⁺.

Inorganica Chimica Acta 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

Paddon, Christopher A. published the artcileCoulometry on the voltammetric timescale: microdisk potential-step chronoamperometry in aprotic solvents reliably measures the number of electrons transferred in an electrode process simultaneously with the diffusion coefficients of the electroactive species, Product Details of C22H18O2, the publication is Electroanalysis (2007), 19(1), 11-22, database is CAplus.

Microdisk, single potential-step chronoamperometry, is applied to a range of organic substrates in the aprotic solvents THF, propylene carbonate, MeCN and the room temperature ionic liquid [C₄dmim][N(Tf)₂] (1-butyl-2,3-dimethylimidazolium bis(trifluoromethylsulfonyl)imide). Fitting of the chronoamperometric transients was achieved using the Shoup and Szabo method. Accurate values for the diffusion coefficients, D, and the number of electron(s) transferred, n, in the electrode process were simultaneously and consistently obtained. This method is generally applicable and reliable for the determination of the number of electrons transferred in faradaic processes uncomplicated by relatively slow coupled homogeneous kinetics. Since the experiment is conducted essentially on typical voltammetric timescales it can be commended as a complementary technique for classical coulometry which is only possible on much longer timescales. The chronoamperometric method is therefore likely to be of greater relevance to the interpretation of voltammetric data.

Electroanalysis published new progress about 2960-93-2. 2960-93-2 belongs to naphthyridine, auxiliary class Naphthalene,Ether,Other MOF ligands,Organic ligands for MOF materials, name is 2,2′-Dimethoxy-1,1′-binaphthalene, and the molecular formula is C22H18O2, Product Details of C22H18O2.

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

Elmore, Eugene published the artcileCorrelation of in vitro chemopreventive efficacy data from the human epidermal cell assay with animal efficacy data and clinical trial plasma levels, Category: naphthyridine, the publication is Journal of Cellular Biochemistry (2005), 95(3), 571-588, database is CAplus and MEDLINE.

The human epidermal cell (HEC) assay, which uses carcinogen exposed normal skin keratinocytes to screen for cancer prevention efficacy, was used to screen possible preventive agents. The endpoints measured were inhibition of carcinogen-induced growth and induction of involucrin, an early marker of differentiation. Sixteen of twenty agents (apigenin, apomine, budesonide, N-(2-carboxyphenyl)retinamide, ellagic acid, ibuprofen, indomethacin, melatonin, (-)-2-oxo-4-thiazolidine carboxylic acid, polyphenon E, resveratrol, β-sitosterol, sulfasalazine, vitamin E acetate, and zileuton) were pos. in at least one of the two assay endpoints. Four agents (4-methoxyphenol, naringenin, palmitoylcarnitine chloride, and silymarin) were neg. in the assay. Nine of the sixteen agents were pos. for both endpoints. Agents that showed the greatest response included: ellagic acid > budesonide, ibuprofen > apigenin, and quinicrine dihydrochloride. Fifty-eight of sixty-five agents that have been evaluated in the HEC assay have also been evaluated in one or more rodent bioassays for cancer prevention and several are in clin. trials for cancer prevention. The assay has an overall predictive accuracy of ∼91.4% for efficacy in rodent cancer prevention irresp. of the species used, the tissue model, or the carcinogen used. Comparison of the efficacious concentrations in vitro to plasma levels in clin. trials show that concentrations that produced efficacy in the HEC assay were achieved in clin. studies for 31 of 33 agents for which plasma levels and/or C_max levels were available. For two agents, 9-cis-retinoic acid (RA) and dehydroepiandrosterone (DHEA), the plasma levels greatly exceeded the highest concentration (HC) found to have efficacy in vitro. Thus, the HEC assay has an excellent predictive potential for animal efficacy and is responsive at clin. achievable concentrations

Journal of Cellular Biochemistry 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, Category: naphthyridine.

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

Li, Jing published the artcilemTORC1-Driven Tumor Cells Are Highly Sensitive to Therapeutic Targeting by Antagonists of Oxidative Stress, Name: Sulindac sulfone, the publication is Cancer Research (2016), 76(16), 4816-4827, database is CAplus and MEDLINE.

MTORC1 is a central signaling node in controlling cell growth, proliferation, and metabolism that is aberrantly activated in cancers and certain cancer-associated genetic disorders, such as tuberous sclerosis complex (TSC) and sporadic lymphangioleiomyomatosis. However, while mTORC1-inhibitory compounds (rapamycin and rapalogs) attracted interest as candidate therapeutics, clin. trials have not replicated the promising findings in preclin. models, perhaps because these compounds tend to limit cell proliferation without inducing cell death. In seeking to address this issue, we performed a high-throughput screen for small mols. that could heighten the cytotoxicity of mTORC1 inhibitors. Here we report the discovery that combining inhibitors of mTORC1 and glutamate cysteine ligase (GCLC) can selectively and efficiently trigger apoptosis in Tsc2-deficient cells but not wild-type cells. Mechanistic investigations revealed that coinhibition of mTORC1 and GCLC decreased the level of the intracellular thiol antioxidant glutathione (GSH), thereby increasing levels of reactive oxygen species, which we determined to mediate cell death in Tsc2-deficient cells. Our findings offer preclin. proof of concept for a strategy to selectively increase the cytotoxicity of mTORC1 inhibitors as a therapy to eradicate tumor cells marked by high mTORC1 signaling, based on cotargeting a GSH-controlled oxidative stress pathway. Cancer Res; 76(16); 4816-27. ©2016 AACR.

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 C20H17FO4S, Name: Sulindac sulfone.

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

Lee, Dae Hee published the artcileHigh-performance low-bandgap conjugated polymers bearing diethynylanthracene units for thin-film transistors, Category: naphthyridine, the publication is Chemical Communications (Cambridge, United Kingdom) (2013), 49(37), 3896-3898, database is CAplus and MEDLINE.

Novel donor-acceptor π-conjugated copolymers, P(DPP-BDT) and P(DPP-ANT), were synthesized in 87-89% yield. Thin-film transistors (TFTs) made from the thermally annealed film of P(DPP-ANT) exhibited much better performance (e.g., μ_max = 1.90 cm² V^-1 s^-1, I_on/off ≈ 10⁶) than those made from the thermally annealed film of P(DPP-BDT).

Chemical Communications (Cambridge, United Kingdom) 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 C18H10, Category: naphthyridine.

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