Category: naphthyridine

Moon, Eun-Yi published the artcileBenzylamide sulindac analogues induce changes in cell shape, loss of microtubules and G₂-M arrest in a chronic lymphocytic leukemia (CLL) cell line and apoptosis in primary CLL cells, Computed Properties of 59973-80-7, the publication is Cancer Research (2002), 62(20), 5711-5719, database is CAplus and MEDLINE.

Given our interest in cyclic nucleotide phosphodiesterase inhibitors in chronic lymphocytic leukemia (CLL), we studied the effects of sulindac sulfone (exisulind), a non-cyclooxygenase-inhibitory end metabolite of the NSAID sulindac that has been reported to inhibit cGMP phosphodiesterases. We focused on a novel benzylamide analog of sulindac sulfone, CP461, which is in clin. trials as a chemotherapeutic agent. As previously reported for colon carcinoma cell lines, we found that CP461 induced a rise in cGMP levels and blocked cell proliferation in the CLL cell line WSU-CLL. Surprisingly, however, cell cycle anal. revealed that CP461 caused G₂-M arrest with an EC₅₀ of 1.1 渭M. G₂-M arrest was associated with phosphorylation of Bcl2 (but not BAD, Bax, or Bcl-XL): both of these end points were abrogated by treatment with a calcium chelator. Although CP461 induces p53 up-regulation, G₂-M arrest and Bcl2 phosphorylation were independent of p53. Because microtubule-active drugs such as vincristine also induced G₂-M arrest and Bcl2 phosphorylation in WSU-CLL, whereas the genotoxic drugs etoposide and doxorubicin did not, we examined the effect of CP461 on microtubules by indirect immunofluorescence microscopy. CP461 eliminated microtubules rapidly, with reduction detected within 30 min of drug treatment. CP461 also induced marked changes in cell shape. Neither sulindac sulfide (a cyclooxygenase inhibitor) nor sulindac sulfone induced G₂-M arrest, Bcl2 phosphorylation, microtubule disassembly, or cell shape changes. Treatment with 30 渭M CP461 induced greater than 50% apoptosis in 10 of 10 primary CLL leukemic cell samples, whereas the same drug concentration had only marginal effects (14% apoptosis) on whole mononuclear cells. Our work demonstrates that addition of a benzylamide moiety to sulindac compounds results in markedly altered pharmacol. properties that may be of use in the therapy of lymphoid malignancies.

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, Computed Properties of 59973-80-7.

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

Kay, Kwang-Yol published the artcileSynthesis and electroluminescent properties of fluorene- and anthracene-derivatives containing novel tetraphenylbenzene moiety, COA of Formula: C18H10, the publication is Molecular Crystals and Liquid Crystals (2004), 167-172, database is CAplus.

2,7-Bis[(2,3,4,5-tetraphenyl)phenyl]-9,9-diethylfluorene (BTPDF) and 2,7-bis[(2,3,4,5-tetraphenyl)phenyl]-9,10-anthracene (BTPA), which consist of a diethylfluorene and an anthracene with two tetraphenylbenzene moieties, were synthesized by Diels-Alder reaction and characterized to investigate electroluminescent (EL) behavior. BTPDF and BTPA showed violet and blue photoluminescence spectra at 400 nm and 456 nm. The device of m-MTDATA (600 脜)/NPB (150 脜)/BTPDF or BTPA (300 脜)/Alq3 (300 脜)/LiF (10 脜)/Al (2000 脜) showed turn-on voltage of 9 V and 13 V and blue and green EL spectrum at 466 nm and 504 nm, resp.

Molecular Crystals and Liquid Crystals 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, COA of Formula: C18H10.

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

Velasco, Manuel I. published the artcileA green alternative to synthetize azo compounds, COA of Formula: C10H9NO4S, the publication is Dyes and Pigments (2011), 90(3), 259-264, database is CAplus.

Different nitrates were used as sources of nitrosonium ion to obtain diazonium salts. Diverse azo compounds were synthesized in acetonitrile giving very good yields and free of byproducts in comparison with traditional synthesis. Among the tested species, the best combination for para red synthesis was nitric acid and gaseous hydrogen chloride.

Dyes and Pigments 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 C15H14O, COA of Formula: C10H9NO4S.

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

Jiang, Jian published the artcileNovel conjugated polymer containing anthracene backbone: the microstructure of polymer composed of 1,4-benzenedithiol with 9,10-diethynylanthracene and isomerization of the polymer and model compounds, COA of Formula: C18H10, the publication is Polymer Journal (Tokyo, Japan) (1990), 22(3), 274-82, database is CAplus.

In order to determine the microstructure of the polymer composed of 1,4-benzenedithiol with 9,10-diethynylanthracene, the model compounds cis– and trans-9,10-bis(phenylthiovinylene)anthracenes were prepared In comparison with the characteristic absorption peaks of vinylene in the model compounds, the microstructure of the polymer was evaluated. Regardless of the initiation mode, UV irradiation, AIBN and none, the cis contents of the polymers were 80-85%. The cis configuration of the polymer isomerized gradually to the trans one with increase of UV irradiation time. The characteristic features of the isomerization were also studied using model compounds The cis isomer of the model compound underwent irreversible isomerization to the trans one by UV irradiation In the presence of a radical source in the reaction system, both the cis and trans isomers can isomerize and reach an equilibrium state after reaction for a sufficient time. The isomerization mechanism was also discussed based on the potential energy diagram.

Polymer Journal (Tokyo, Japan) 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, COA of Formula: C18H10.

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

Weber, E. published the artcileBenzo condensed crown ethers containing 1,8-naphthyridine or 4-pyridone units. Synthesis and complex formation with organic guest molecules, SDS of cas: 14903-78-7, the publication is Journal fuer Praktische Chemie/Chemiker-Zeitung (1995), 337(6), 451-5, database is CAplus.

New crown compounds, e.g., I, comprising, beside o-phenylene groups, 1,8-naphthyridine or 4-pyridone groups as characteristic building units are synthesized. They form numerous stoichiometric crystalline complexes with uncharged organic mols. including alcs., nitro compounds and other dipolar-aprotic solvents, as well as cyclic ethers and aromatic hydrocarbons. Properties of complex formation and host-guest stoichiometries are discussed in comparison with parent host analogs.

Journal fuer Praktische Chemie/Chemiker-Zeitung 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 C26H41N5O7S, SDS of cas: 14903-78-7.

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

Belyaev, Andrey published the artcileSolution versus solid-state dual emission of the Au(I)-alkynyl diphosphine complexes via modification of polyaromatic spacers, Safety of 9,10-Diethynylanthracene, the publication is New Journal of Chemistry (2019), 43(35), 13741-13750, database is CAplus.

Single mol. luminophores capable of multiple emissions are essential for the development of new materials with unconventional photophys. behavior. In this work, a family of diphosphine ligands PPh₂-PAH-PPh₂ with variable polyaromatic hydrocarbon (PAH) spacers (PAH = 9,10-anthracene L1, 1,4-naphthalene L2, 2,6-naphthalene L3, and their diethynyl congeners L4–L6) were employed to prepare gold(I) complexes (RC₂Au)PPh₂-PAH-PPh₂(AuC₂R) (1–22), containing a selection of alkynyl groups. Investigation of their optical properties indicates that compounds with anthracene-based diphosphines (1–4 and 13–16) display only ¹IL (蟺蟺*) fluorescence with 桅_em up to 93%. The naphthalene and diethynyl-naphthalene diphosphine complexes (5–12 and 17–22), however, demonstrate panchromatic emission in the solid state and in solution featuring well-separated low and high energy signals, which originate from ¹IL (蟺蟺*) and ³IL (蟺蟺*) transitions along with certain contribution from metal to ligand and ligand to ligand charge transfers.

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 C18H10, Safety of 9,10-Diethynylanthracene.

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

Li, Yongjun published the artcileIntramolecular triplet energy transfer in anthracene-based platinum acetylide oligomers, Category: naphthyridine, the publication is Journal of Physical Chemistry B (2013), 117(30), 9025-9033, database is CAplus and MEDLINE.

Platinum acetylide oligomers that contain an anthracene moiety have been synthesized and subjected to photophys. characterization. Spectroscopic measurement and DFT calculations reveal that both the singlet and triplet energy levels of the anthracene segment are lower than those of the platinum acetylide segment. Thus, the platinum acetylide segment acts as a sensitizer to populate the triplet state of the anthracene segment via intramol. triplet-triplet energy transfer. The objective of this work is to understand the mechanisms of energy-transfer dynamics in these systems. Fluorescence quenching and the dominant triplet absorption that arises from the anthracene segment in the transient absorption spectrum of Pt4An give clear evidence that energy transfer adopts an indirect mechanism, which begins with singlet-triplet energy transfer from the anthracene segment to the platinum acetylide segment followed by triplet-triplet energy transfer to the anthracene segment.

Journal of Physical Chemistry B 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

Sfoungaristos, Stavros published the artcileNeoadjuvant chemotherapy prior to radical prostatectomy for patients with high-risk prostate cancer: a systematic review, Synthetic Route of 59973-80-7, the publication is Chemotherapy Research and Practice (2013), 386809, 7 pp., database is CAplus and MEDLINE.

High-risk prostate cancer represents a pretentious clin. problem since a significant number of its patients will relapse and progress after radical prostatectomy. Neoadjuvant chemotherapy may be valuable since its efficacy in hormone-resistant prostate cancer has been established. In this paper, we report studies of neoadjuvant chemotherapies that have been used in high-risk patients prior to radical prostatectomy. Even though the results regarding the prognostic surrogates are not significant, the effects on clin. and pathol. outcomes are promising, while toxicity in most of the studies is in the expected field.

Chemotherapy Research and Practice 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 C42H63O3P, Synthetic Route of 59973-80-7.

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

Pangburn, Heather A. published the artcileSulindac metabolites inhibit epidermal growth factor receptor activation and expression, Related Products of naphthyridine, the publication is Journal of Carcinogenesis (2005), No pp. given, database is CAplus and MEDLINE.

Background: Regular use of nonsteroidal anti-inflammatory drugs (NSAIDs) is associated with a decreased mortality from colorectal cancer (CRC). NSAIDs induce apoptotic cell death in colon cancer cells in vitro and inhibit growth of neoplastic colonic mucosa in vivo however, the biochem. mechanisms required for these growth inhibitory effects are not well defined. We previously reported that metabolites of the NSAID sulindac downregulate extracellular-signal regulated kinase 1/2 (ERK1/2) signaling and that this effect is both necessary and sufficient for the apoptotic effects of these drugs. The goal of this project was to specifically test the hypothesis that sulindac metabolites block activation and/or expression of the epidermal growth factor (EGF) receptor (EGFR). Methods: HT29 human colon cancer cells were treated with EGF, alone, or in the presence of sulindac sulfide or sulindac sulfone. Cells lysates were assayed by immunoblotting for phosphorylated EGFR (pEGFR, pY1068), total EGFR, phosphorylated ERK1/2 (pERK1/2), total ERK1/2, activated caspase-3, and 伪-tubulin. Results: EGF treatment rapidly induced phosphorylation of both EGFR and ERK1/2 in HT29 colon cancer cells. Pretreatment with sulindac metabolites for 24h blocked EGF-induced phosphorylation of both EGFR and ERK1/2 and decreased total EGFR protein expression. Under basal conditions, downregulation of pEGFR and total EGFR was detected as early as 12h following sulindac sulfide treatment and persisted through at least 48h. Sulindac sulfone induced downregulation of pEGFR and total EGFR was detected as early as 1h and 24h, resp., following drug treatment, and persisted through at least 72h. EGFR downregulation by sulindac metabolites was observed in three different CRC cell lines, occurred prior to the observed downregulation of pERK1/2 and induction of apoptosis by these drugs, and was not dependent of caspase activation. Conclusion: These results suggest that downregulation of EGFR signaling by sulindac metabolites may occur, at least in part, by inhibiting activation and expression of EGFR. Inhibition of EGFR signaling may account for part of the growth inhibitory and chemopreventive effects of these compounds

Journal of Carcinogenesis 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

Paudler, William W. published the artcileNaphthyridine chemistry. VIII. Mass spectra of the 1,x-naphthyridines and some of their methyl derivatives, Name: 2,7-Dimethyl-1,8-naphthyridine, the publication is Journal of Heterocyclic Chemistry (1967), 4(4), 547-54, database is CAplus.

The mass spectra of the four parent 1,x-naphthyridines, the 2-, 3-, and 4-monomethyl-1,5-, 1,6-, and 1,8-naphthyridines, seven dimethyl-1,8-naphthyridines, and one trimethyl-1,8-naphthyridine are reported. Evidence for an azatropylium ion intermediate in the fragmentation of the methyl compounds is presented. The fragmentation modes of the naphthyridines are similar to those for the quinolines in addition to several new processes.

Journal of Heterocyclic 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, Name: 2,7-Dimethyl-1,8-naphthyridine.

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