Month: November 2022

Lim, Soo-Jeong published the artcileAlpha-tocopheryl succinate sensitizes human colon cancer cells to exisulind-induced apoptosis, Name: Sulindac sulfone, the publication is Apoptosis (2007), 12(2), 423-431, database is CAplus and MEDLINE.

Sulindac sulfone (also known as exisulind) and its chem. derivatives are promising anticancer agents capable of inducing apoptosis in a variety of malignant cell types with minimal toxicity to normal cells. Here, we tested the ability of alpha-tocopheryl succinate (TOS), another promising anticancer agent, to sensitize colon cancer cells to exisulind-induced apoptosis. We found that sub-apoptotic doses of TOS greatly enhanced exisulind-induced growth suppression and apoptosis in the HCT116, LoVo and SNU-C4 human colon cancer cell lines. Our results revealed that this was accounted for primarily by an augmented cleavage of poly(ADP-ribose) polymerase (PARP) and enhanced activation of caspase-8, -9 and -3. Pretreatment with z-VAD-FMK (a pan-caspase inhibitor), z-IETD-FMK (a caspase-8 inhibitor) or z-LEHD-FMK (a caspase-9 inhibitor) blocked TOS and exisulind cotreatment-induced PARP cleavage and apoptosis. Furthermore, TOS/exisulind cotreatment induced JNK phosphorylation, while pretreatment with SP600151 (a JNK inhibitor) partially blocked cotreatment-induced caspase-dependent PARP cleavage and apoptosis. Taken together, these findings indicate that TOS sensitizes human colon cancer cells to exisulind-induced apoptosis. Apoptotic synergy induced by exisulind plus TOS seems likely to be mediated through a mechanism involving activation of caspases and JNK.

Apoptosis 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

Lim, Soo-Jeong published the artcileP38MAPK inhibitor SB203580 sensitizes human SNU-C4 colon cancer cells to exisulind-induced apoptosis, Application In Synthesis of 59973-80-7, the publication is Oncology Reports (2006), 16(5), 1131-1135, database is CAplus and MEDLINE.

Sulindac sulfone (exisulind), is a promising anti-cancer agent because of its ability to induce apoptosis in a variety of malignant cell types and its minimal toxicity to normal cells. The induction of apoptosis is thought to account for the growth inhibitory effect of exisulind. The mitogen-activated protein kinase (MAPK) cascade has been implicated in the regulation of apoptosis in response to exisulind. With human SNU-C4 colon cancer cells that were much more resistant to exisulind than other colon cancer cells, in this study, we investigated whether the modulation of MAPK activity by using selective MAPK inhibitors can contribute to sensitizing SNU-C4 cells to exisulind. Exisulind (400 and 600 渭M) slightly increased the phosphorylation of pERK1/2 but pretreatment with the pERK1/2 inhibitor PD98059 did not significantly change the apoptotic response of SNU-C4 cells. The same doses of exisulind increased the phosphorylation of p38MAPK, and pretreatment with the p38MAPK inhibitor SB203580 significantly potentiated growth inhibition and apoptosis induced by exisulind in SNU-C4 cells. We further found that apoptosis induced by a combination of exisulind and SB203580 was mediated through caspase activation. Collectively, our findings indicate that selective p38MAPK inhibitors potentiate apoptosis induction by exisulind in SNU-C4 cells. Such combinations may provide a more effective and less toxic strategy for the prevention or treatment of colon cancer.

Oncology Reports 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

Kwak, Min Seob published the artcileNovel candidate drugs in anti-tumor necrosis factor refractory Crohn’s diseases: in silico study for drug repositioning, Recommanded Product: Sulindac sulfone, the publication is Scientific Reports (2020), 10(1), 10708, database is CAplus and MEDLINE.

Abstract: Biologicals like anti-tumor necrosis factor (TNF) therapy for Crohn’s disease (CD) are safe and effective but there is a significant rate of primary and secondary nonresponse in the patients. In this study, we applied a computational approach to discover novel drug therapies for anti-TNF refractory CD in silico. We use a transcriptome dataset (GSE100833) for the anti-TNF refractory CD patients from NCBI GEO. After co-expression anal., we specifically investigated the extent of protein-protein interactions among genes in clusters based on a protein-protein interaction database, STRING. Pathway anal. was performed using the clEnrich function based on KEGG gene sets. Co-expressed genes in cluster 1, 2, 3, 4, up or down-regulated genes and all differentially expressed genes are highly connected. Among them, cluster 1, which is highly enriched for chemokine signaling, also showed enrichment for cytokine-cytokine receptor interaction and identifies several drugs including cyclosporin with known efficacy in CD. Vorinostat, histone deacetylase inhibitors, and piperlongumine, which is known to have inhibitory effect on activity of NF-kB, were also identified. Some alkaloids were also selected as potential therapeutic drugs. These finding suggest that they might serve as a novel therapeutic option for anti-TNF refractory CD and support the use of public mol. data and computational approaches to discover novel therapeutic options for CD.

Scientific Reports 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

Wong, Wai-Yeung published the artcileSynthesis and characterization of new oligoacetylenic silanes, Formula: C18H10, the publication is New Journal of Chemistry (2002), 26(3), 354-360, database is CAplus.

Synthetic routes to a series of novel oligoacetylenic silanes with or without (hetero)aromatic bridges have been developed. The compound Me₃SiC顚咰Si(Ph)₂C顚咰SiMe₃ was first prepared, which was selectively desilylated with CaCO₃ in methanol at room temperature to afford the mono-protected bis(alkynyl)silane Me₃SiC顚咰Si(Ph)₂C顚咰H in moderate yield. Treatment of this mono-protected species with ⁿBuLi, followed by silylation with Ph₂SiCl₂, gives a good yield of Me₃SiC顚咰Si(Ph)₂C顚咰Si(Ph)₂C顚咰Si(Ph)₂C顚咰SiMe₃, with alternating silicon and acetylene units. A range of linear silicon-linked oligoalkynes containing phenylene, bithienylene and anthrylene rings, HC顚咰RC顚咰Si(Ph)₂C顚咰RC顚咰H and HC顚咰RC顚咰Si(Ph)₂C顚咰RC顚咰Si(Ph)₂C顚咰RC顚咰H (R = 1,4-phenylene, 5,5′-bithienylene or 9,10-anthrylene), were synthesized by condensation reactions of Ph₂SiCl₂ with the components obtained in situ from a HC顚咰RC顚咰H-ⁿBuLi mixture in THF and the products were isolated by chromatog. on silica. All these new compounds have been characterized by IR, ¹H and ¹³C NMR and UV/VIS spectroscopies and mass spectrometry. The single-crystal x-ray structure of HC顚咰(p-C₆H₄)C顚咰Si(Ph)₂C顚咰(p-C₆H₄)C顚咰Si(Ph)₂C顚咰(p-C₆H₄)C顚咰H has been determined, showing that two silicon atoms and six acetylene units constitute the backbone of the mol.

New Journal of Chemistry 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 C19H14FN3O3S, Formula: C18H10.

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

Andrews, Michael published the artcileA luminescent rhenium(I) complex of 2,7-dimethyl-1,8-naphthyridine: Synthesis, spectroscopy and X-ray crystal structure, Category: naphthyridine, the publication is Transition Metal Chemistry (Dordrecht, Netherlands) (2009), 34(5), 493-497, database is CAplus.

2,7-Dimethyl-1,8-naphthyridine (L¹) reacts with pentacarbonylchlororhenium in toluene or chloroform to give the target complex fac-{ReCl(CO)₃(L¹)}. X-ray crystallog. data were obtained for fac-{ReCl(CO)₃(L¹)}. The structural and ¹H NMR data suggest that the ligand coordinates to the rhenium in a bidentate fashion in both solid and solution states. The complex also is luminescent in both solution and solid states. The fluxionality of the ligand in solution causes ligand-centered emission to be observed in solution, whereas only ³MLCT emission was observed in the solid state. Although the complex was air-stable, the lability of L¹ was studied in ¹H NMR experiments where CD₃OD induced complete ligand dissociation over 24 h, and also in reaction of fac-{ReCl(CO)₃(L¹)} with one equivalent of 2,2′-bipyridine in chloroform which resulted in quant. ligand exchange.

Transition Metal Chemistry (Dordrecht, Netherlands) 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, Category: naphthyridine.

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

Karafiloglou, Padeleimon published the artcileComparing electron (de)localization in the through benzene and anthracene charge transfer, Synthetic Route of 18512-55-5, the publication is Chemical Physics (2003), 289(2-3), 231-242, database is CAplus.

The contrasting behavior of benzene and anthracene in the through 蟺-system passing of a (+) charge is examined by considering para-diethynylbenzene and para-diethynylanthracene spacers. The (de)localization of their bonds in both neutral and cationic forms are compared by a two-electron population anal.; the electron-pair distributions are calculated in orbital spaces appropriate for population anal., as the natural AOs, in which two-electron correlations are also studied. When the spacer involves benzene, then its oxidation causes a reorganization of electron pairs towards a pronounced quinoid bond (de)localization, which induces analogous bond deformations; on the contrary, in the case of anthracene, a similar quinoid (de)localization (and the corresponding bond deformation) is impeded, due to the possibility of addnl. delocalization on its central ring. As shown, these electron-pair reorganizations are the driving force for the corresponding geometrical deformations.

Chemical Physics 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, Synthetic Route of 18512-55-5.

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

Patra, Kamaless published the artcileA Protic Mn(I) Complex Based on a Naphthyridine-N-oxide Scaffold: Protonation/Deprotonation Studies and Catalytic Applications for Alkylation of Ketones, Category: naphthyridine, the publication is Organometallics (2022), 41(14), 1836-1846, database is CAplus.

A Mn(I) complex (1) bearing a proton responsive hydroxy unit on 1,8-naphthyridine-N-oxide scaffold (L¹H) was synthesized. The mol. structure of 1 revealed the lactim form of the ligand. The corresponding deprotonated lactam complexes [18-C-6-K路2] and 3 were prepared and structurally characterized. The acid-base equilibrium between the lactim and lactam forms was studied by ¹H NMR and UV-visible spectra. The catalytic efficiency of 1 was evaluated by performing 伪-alkylation reaction of ketones with primary alcs. The scope of the 伪-alkylation reaction is broad in terms of both ketones and alcs. The efficacy of the protic catalyst is demonstrated in the alkylation of the bioactive steroids progesterone and pregnenolone. A controlled catalyst [Mn(L²)(CO)₃Br] (4), which is structurally similar to 1 but devoid of the proton responsive hydroxy unit, shows significantly reduced catalytic efficiency validating the crucial role of the hydroxy functionality in 1. Kinetic study, control reactions, and D labeling experiments were conducted to gain mechanistic insights.

Organometallics 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, Category: naphthyridine.

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

Kuehl, Gwendolyn E. published the artcileGlucuronidation of nonsteroidal anti-inflammatory drugs: Identifying the enzymes responsible in human liver microsomes, Application In Synthesis of 59973-80-7, the publication is Drug Metabolism and Disposition (2005), 33(7), 1027-1035, database is CAplus and MEDLINE.

Nonsteroidal anti-inflammatory drugs (NSAIDs), used for the treatment of pain and inflammation, are eliminated primarily through conjugation with polar sugar moieties to form glucuronides. Glucuronidation is catalyzed by the UDP-glucuronosyltransferases (UGT) superfamily. An inverse relationship may exist between glucuronidation activity and NSAID efficacy; however, specific UGTs catalyzing conjugation of the structurally diverse NSAIDs have yet to be identified systematically. Therefore, NSAID glucuronidation activity by 12 individually expressed UGTs was investigated by liquid chromatog.-tandem mass spectrometry. The relative rates of NSAID glucuronidation varied among UGT enzymes examined, demonstrating specificity of the individual UGTs toward selected NSAIDs. Kinetic parameters were determined for expressed UGT Supersomes and compared with parameters determined in pooled human liver microsomes (HLMs). Comparison of K_m values suggested roles for UGTs 1A3 and 2B7 in indene glucuronidation and UGTs 1A9, 2B4, and 2B7 in profen glucuronidation. Inhibitory studies in pooled HLMs support the role of UGTs 1A1, 1A3, 1A9, 2B4, and 2B7 in the glucuronidation of ibuprofen, flurbiprofen, and ketoprofen. Bilirubin did not inhibit indomethacin or diclofenac glucuronidation, suggesting that UGT1A1 was not involved in catalysis. Imipramine did not inhibit glucuronidation of sulindac, sulindac sulfone, indomethacin, or naproxen in pooled HLMs, suggesting that UGT1A3 was not a principal hepatic catalyst. Nevertheless, multiple UGT enzymes, most notably UGTs 1A1, 1A9, 2B4, and 2B7, seem to be involved in the hepatic catalysis of NSAID glucuronidation.

Drug Metabolism and Disposition 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

Raj Sinha, Deo published the artcileNaphthyridines reactivity of methyl groups: new cyanine dyes from 2,7-dimethyl- and 4,7-dimethyl-1,8-naphthyridines, Quality Control of 14903-78-7, the publication is Journal of the Indian Chemical Society (1979), 56(2), 164-7, database is CAplus.

The reactivity of the 4-Me in 4,7-dimethyl-1,8-naphthyridine (I) [14759-23-0] is greater than the 7-Me towards condensation with m-nitrobenzladehyde [99-61-6]. Cyanine and styryl dyes derived from I and from 2,7-dimethyl-1,8-naphthyridine [14903-78-7] were prepared and their structures established. The trimethine dyes were found to be useless as sensitizers for Ag halide emulsions.

Journal of the Indian Chemical Society 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, Quality Control of 14903-78-7.

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

Drahonovsky, Dusan published the artcilePinene-fused chiral N-ethylpyridinum room temperature molten salts, COA of Formula: C22H18O2, the publication is Heterocycles (2005), 65(9), 2169-2179, database is CAplus.

New chiral room temperature molten salts (ionic liquids) based on the pinene-pyridinium unit associated with triflate or trifluoroacetate anions I (X^– = CF₃SO₂^–, CF₃CO₂^–) were prepared The thermal behavior of these salts was observed by DSC and solventless ¹H NMR spectrum, whereas the diastereomeric interactions were studied by test asym. reactions, GC, CD spectroscopy, and ¹⁹F NMR spectra. X-ray structure of iodide intermediate is presented.

Heterocycles 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, COA of Formula: C22H18O2.

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