Month: November 2022

Gribkov, Denis V. published the artcileSynthesis and characterization of new biphenolate and binaphtholate rare-earth-metal amido complexes: Catalysts for asymmetric olefin hydroamination/cyclization, Name: 2,2′-Dimethoxy-1,1′-binaphthalene, the publication is Chemistry – A European Journal (2003), 9(19), 4796-4810, database is CAplus and MEDLINE.

Monomeric diolate amido yttrium complexes [Y{diolate}{N(SiHMe₂)₂}(THF)₂] can be prepared in good yield by treating [Y{N(SiHMe₂)₂}₃(THF)₂] with either 3,3′-di-tert-butyl-5,5′,6,6′-tetramethyl-1,1′-biphenyl-2,2′-diol (H₂(Biphen)), 3,3′-bis(2,4,6-triisopropylphenyl)-2,2′-dihydroxy-1,1′-dinaphthyl (H₂(Trip₂BINO)) or 3,3′-bis(2,6-diisopropylphenyl)-2,2′-dihydroxy-1,1′-dinaphthyl (H₂(Trip₂BINO)) in racemic and enantiopure form. The racemic complex [Y(biphen){N(SiHMe₂)₂}(THF)₂] dimerizes upon heating to give the heterochiral complex (R,S)-[Y(biphen){N(SiHMe₂)₂}(THF)]₂. The corresponding dimeric heterochiral lanthanum complex was the sole product in the reaction of H₂(Biphen) with [La{N(SiHMe₂)₂}₃(THF)₂]. Single-crystal x-ray diffraction of both dimeric complexes revealed that the two Ln(biphen){N(SiHMe₂)₂}(THF) fragments are connected through bridging phenolate groups of the biphenolate ligands. The two different phenolate groups undergo an intramol. exchange process in solution leading to their equivalence on the NMR timescale. All complexes were active catalysts for the hydroamination/cyclization of aminoalkynes and aminoalkenes at elevated temperature, with [Y((R)-dip₂bino){N(SiHMe₂)₂}(THF)₂] being the most active one giving enantioselectivities of up to 57% ee. Kinetic resolution of 2-aminohex-5-ene proceeded with this catalyst with 6.4:1 trans selectivity to give 2,5-dimethylpyrrolidine with a k_rel of 2.6.

Chemistry – A European Journal 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, Name: 2,2′-Dimethoxy-1,1′-binaphthalene.

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

Huang, Wei published the artcileHydrogel formulation of phosphosulindac allows once-a-day ocular dosing and limits its biodistribution to the anterior chamber: Application to dry eye disease treatment, HPLC of Formula: 59973-80-7, the publication is Journal of Drug Delivery Science and Technology (2022), 102961, database is CAplus.

We report the pharmacokinetics, biodistribution and metabolism of phospho-sulindac (PS) in a hydrogel formulation efficacious in dry eye disease (DED) administered once daily. PS 0.2% and 0.7% was studied in Dutch-Belted black and New Zealand white rabbits with and without DED. Levels of PS and its metabolites were determined by HPLC. The two rabbit strains gave similar results. PS and its metabolites were limited to the anterior chamber of the eye and undetectable in peripheral blood. DED did not affect the PK, biodistribution or metabolism of PS. Drug levels were dose dependent. PS had a rapid uptake (Tmax 15-30 min) and short t1/2 (0.6-0.9 h), being undetectable at 8h. Of the anterior chamber tissues, cornea and conjunctiva had >90% of the total PS. PS metabolism was rapid and complete, generating all its known in vivo metabolites, except for glucuronidation products. Rabbits with DED had 1.8-fold longer precorneal residence time of PS. The prolonged efficacy of PS despite its limited presence in ocular tissues suggests a vigorous downstream action suppressing ocular surface inflammation of DED. The properties of this formulation, especially the combination of superior efficacy with once-a-day dosing are a major improvement over previous formulations for the treatment of DED.

Journal of Drug Delivery Science and Technology 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, HPLC of Formula: 59973-80-7.

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

Hua, Si-Kai published the artcileDilithium tetrachlorocuprate(II) catalyzed oxidative homocoupling of functionalized Grignard reagents, COA of Formula: C22H18O2, the publication is Synthesis (2013), 45(4), 518-526, database is CAplus.

An efficient procedure is described for the oxidative homocoupling of functionalized Grignard reagents using a catalytic amount of dilithium tetrachlorocuprate(II) (CuLi₂Cl₄) in the presence of pure oxygen gas. This method is applied successfully to a variety of aryl, heteroaryl, alkyl, alkenyl and alkynyl halides, which are converted into the corresponding homocoupled products in good to excellent yields.

Synthesis 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

Liang, Xiao published the artcileIdentification of Core Genes and Potential Drugs for Castration-Resistant Prostate Cancer Based on Bioinformatics Analysis, Recommanded Product: Sulindac sulfone, the publication is DNA and Cell Biology (2020), 39(5), 836-847, database is CAplus and MEDLINE.

Prostate cancer (PCa) is a common malignant tumor in elderly men worldwide. Most primary PCas inevitably progress into castration-resistant prostate cancer (CRPC) after androgen deprivation therapy. The mechanisms contributing to this progression are still controversial. In this study, functional module genes, DNA methylations, core regulators, and potential drugs in primary PCa and CRPC were explored by integrating a series of bioinformatics analyses. First, 588 differentially expressed genes (DEGs) were identified. Combined with related genes, protein-protein interaction networks were constructed, and 22 and 14 significant modules were identified in primary PCa and CRPC, resp. More DEGs were identified in differentially methylated genes in CRPC modules. The hub genes in CRPC included CDC20 and CDK1. Moreover, core noncoding RNAs and transcription factors that significantly regulate CRPC modules were identified, including TUG1, MALAT1, E2F3, and MED1. Finally, the prediction of potential drugs for primary PCa and CRPC was also performed. Exisulind and phosphodiesterase-4 inhibitors were predicted as potential drugs for CRPC. The results of this study provide a new way for biologists and pharmacists to understand the potential mol. mechanisms of CRPC and also provide valuable references for drug redirection and new drug development for PCa.

DNA and Cell Biology 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

Tang, Yong-Jun published the artcileEffects of FMO3 polymorphisms on pharmacokinetics of sulindac in Chinese healthy male volunteers, COA of Formula: C20H17FO4S, the publication is BioMed Research International (2017), 4189678/1-4189678/7, database is CAplus and MEDLINE.

Sulindac is a nonsteroidal anti-inflammatory drug, which is clin. used for the ailments of various inflammations. This study investigated the allele frequencies of FMO3 E158K and E308G and evaluated the influences of these two genetic polymorphisms on the pharmacokinetics of sulindac and its metabolites in Chinese healthy male volunteers. Eight FMO3 wild-type (FMO3 HHDD) subjects and seven FMO3 homozygotes E158K and E308G mutant (FMO3 hhdd) subjects were recruited from 247 healthy male volunteers genotyped by PCR-RFLP method. The plasma concentrations of sulindac, sulindac sulfide, and sulindac sulfone were determined by UPLC, while the pharmacokinetic parameters of the two different FMO3 genotypes were compared with each other. The frequencies of FMO3 E158K and E308G were 20.3% and 20.1%, resp., which were in line with Hardy-Weinberg equilibrium (D’ = 0.977, r2 = 0.944). The mean values of Cmax, AUC0-24, and AUC0-âˆ?of sulindac were significantly higher in FMO3 hhdd group than those of FMO3 HHDD group (P < 0.05), while the pharmacokinetic parameters except Tmax of sulindac sulfide and sulindac sulfone showed no statistical difference between the two groups. The two FMO3 mutants were in close linkage disequilibrium and might play an important role in the pharmacokinetics of sulindac in Chinese healthy male volunteers.

BioMed Research International 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 C16H12O, COA of Formula: C20H17FO4S.

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

Morisue, Mitsuhiko published the artcileA metal-lustrous porphyrin foil, Related Products of naphthyridine, the publication is Chemical Communications (Cambridge, United Kingdom) (2017), 53(77), 10703-10706, database is CAplus and MEDLINE.

A metal-lustrous, self-standing film, i.e., porphyrin foil, was formed from a glass-forming polymeric porphyrin. The amorphous glass nature of the porphyrin foil played a key role in spontaneously producing a smooth surface. Its sharp contrast in intense absorption and specular light reflection at each wavelength provided a brilliant metallic luster.

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, Related Products of naphthyridine.

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

Bailey, Andrew James published the artcileSelf-assembly into infinite tapes by 2,7-disubstituted-1,8-naphthyridines in the solid state, Application of 2,7-Dimethyl-1,8-naphthyridine, the publication is CrystEngComm (2010), 12(12), 4074-4079, database is CAplus.

2,7-Disubstituted-1,8-naphthyridine derivatives have been found to self-assemble into infinite 1-dimensional tapes in the solid state in a manner similar to that seen previously for their 2,6-disubstituted pyridine analogs.

CrystEngComm 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, Application of 2,7-Dimethyl-1,8-naphthyridine.

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

Vila, Carlos published the artcilePalladium-Catalysed Direct Cross-Coupling of Organolithium Reagents with Aryl and Vinyl Triflates, SDS of cas: 152873-79-5, the publication is Chemistry – A European Journal (2014), 20(41), 13078-13083, database is CAplus and MEDLINE.

A palladium-catalyzed cross-coupling of organolithium reagents with aryl and vinyl triflates is presented. The reaction proceeds at 50 or 70 °C with short reaction times, and the corresponding products are obtained with moderate to high yields, with a variety of alkyl and (hetero)aryl lithium reagents. E.g., in presence of Pd₂(dba)₃ and DavePhos, cross-coupling of butyllithium and 2-naphthyl triflate gave 81% 2-butylnaphthalene.

Chemistry – A European Journal 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 C25H47NO8, SDS of cas: 152873-79-5.

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

Aono, Yuichi published the artcileSulindac sulfone inhibits the mTORC1 pathway in colon cancer cells by directly targeting voltage-dependent anion channel 1 and 2, Computed Properties of 59973-80-7, the publication is Biochemical and Biophysical Research Communications (2018), 505(4), 1203-1210, database is CAplus and MEDLINE.

Sulindac sulfone is a metabolite of sulindac, a non-steroidal anti-inflammatory drug (NSAID), without anti-inflammatory ability. However, sulindac sulfone has been reported to significantly reduce polyps in patients with colorectal adenomatous polyposis in clin. trials. Thus, sulindac sulfone is expected to be useful for the chemoprevention of neoplasia with few side effects related to anti-inflammatory ability. To date, the mol. targets of sulindac sulfone have not yet fully investigated. Therefore, in order to newly identify sulindac sulfone-binding proteins, we generated sulindac sulfone-fixed FG beads and purified sulindac sulfone-binding proteins from human colon cancer HT-29 cells and We identified mitochondrial outer membrane proteins voltage-dependent anion channel (VDAC) 1 and VDAC2 as novel mol. targets of sulindac sulfone, and sulindac sulfone directly bound to both VDAC1 and VDAC2. Double knockdown of VDAC1 and VDAC2 by siRNA inhibited growth and arrested the cell cycle at G1 phase in HT-29 cells. Depletion of VDAC1 and VDAC2 also inhibited the mTORC1 pathway with a reduction in cyclin D1. Interestingly, these effects were consistent with those of sulindac sulfone against human colon cancer cells, suggesting that sulindac sulfone neg. regulates the function of VDAC1 and VDAC2. In the present study, our data suggested that VDAC1 and VDAC2 are direct targets of sulindac sulfone which suppresses the mTORC1 pathway and induces G1 arrest.

Biochemical and Biophysical Research Communications 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

Mathew, Bini published the artcileDiverse amide analogs of sulindac for cancer treatment and prevention, HPLC of Formula: 59973-80-7, the publication is Bioorganic & Medicinal Chemistry Letters (2017), 27(20), 4614-4621, database is CAplus and MEDLINE.

Sulindac is a non-steroidal anti-inflammatory drug (NSAID) that has shown significant anticancer activity. Sulindac sulfide amide possessing greatly reduced COX-related inhibition relative to sulindac displayed in vivo antitumor activity that was comparable to sulindac in a human colon tumor xenograft model. Inspired by these observations, a panel of diverse sulindac amide derivatives have been synthesized and their activity probed against three cancer cell lines (prostate, colon and breast). A neutral analog, compound 79 ((Z)-N-benzyl-2-(5-fluoro-2-methyl-1-(4-(methylsulfinyl)benzylidene)-1H-inden-3-yl)acetamide) was identified with comparable potency relative to lead 1 and activity against a panel of lymphoblastic leukemia cell lines. Several new series also show good activity relative to the parent , including five analogs that also possess nanomolar inhibitory potencies against acute lymphoblastic leukemia cells. Several new analogs identified may serve as anticancer lead candidates for further development.

Bioorganic & Medicinal Chemistry Letters 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, HPLC of Formula: 59973-80-7.

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