Category: 104-01-8

Zasedateleva, Olga A. published the artcilePCR incorporation of dUMPs modified with aromatic hydrocarbon substituents of different hydrophilicities: Synthesis of C5-modified dUTPs and PCR studies using Taq, Tth, Vent (exo-) and Deep Vent (exo-) polymerases, Recommanded Product: 4-Methoxyphenylacetic acid, the main research area is substituent effect DNA duplex preparation; dUMP aromatic hydrocarbon hydrophilicity synthesis PCR dna polymerase; Aromatic hydrocarbon groups; C5-modified dUTPs; Hydrophilicity; Modified DNA; PCR incorporation.

Deoxyuridine triphosphate derivatives (dUTPs) modified at the C5 position of the pyrimidine ring with various aromatic hydrocarbon substituents of different hydrophilicities have been synthesized. The aromatic hydrocarbon substituents were attached to dUTPs via a CH=CH-CH2-NHCO-CH2 linker. The efficiency of the PCR incorporation of modified dUMPs using Taq, Tth, Vent (exo-) and Deep Vent (exo-) polymerases and a model DNA template containing one, two and three adjacent adenine nucleotides at three different sites within the sequence was investigated. For all the polymerases used, the yield of the modified PCR product was significantly increased with increasing hydrophilicity of the aromatic hydrocarbon substituent. In particular, for the above polymerases, the efficiency of the incorporation of dUMPs modified with the most hydrophilic of the studied aromatic hydrocarbon substituents, a 4-hydroxyphenyl residue, was 60-85% of the efficiency of dTMP incorporation. At the same time, the relative efficiencies of the incorporation of dUMPs modified with 2-, 4-methoxyphenyl, Ph and 4-nitrophenyl substituents ranged from 20 to 50% and were 2-18% for the 1-naphthalene and 4-biphenyl groups, which were the most hydrophobic of the studied aromatic hydrocarbon substituents.

Bioorganic Chemistry published new progress about Nucleotides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Recommanded Product: 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Peczkowski, Gary R. published the artcile2,7-Diazabicyclo[2.2.1]heptanes: novel asymmetric access and controlled bridge-opening, Safety of 4-Methoxyphenylacetic acid, the main research area is diazabicycloheptane preparation; oxoalkyl triketopiperazine enantioselective preparation rearrangement; triketopiperazine enone Michael addition organocatalyst.

An efficient method was developed for the asym. synthesis of oxoalkyl triketopiperazines I [R = H, Me, Et, Ph; Ar = Ph, 4-BrC6H4, 2-furanyl, etc.] via organocatalyzed Michael addition of triketopiperazines to enones in high yields and enantiomeric ratio. These triketopiperazines I underwent rearrangement to afford 2,7-diazabicyclo[2.2.1]heptanes II and further modification delivered products possessing natural product scaffolds including prolinamide and harmicine.

Chemical Communications (Cambridge, United Kingdom) published new progress about Enantioselective synthesis. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Safety of 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Sbaraglini, Maria L. published the artcileLipase catalyzed synthesis of alkyl phenylacetates with anticonvulsant activity, SDS of cas: 104-01-8, the main research area is alkyl phenylacetate preparation mol docking anticonvulsant; phenylacetic acid esterification lipase catalyst.

Despite the wide spectra of available antiepileptic drugs, one third of the patients still suffer from drug-resistant epilepsy, justifying the ongoing search of novel therapies. The anticonvulsant activity of Pr 4-hydroxybenzoate was previously identified through in silico screening. Here, Candida antarctica B (CAL B) lipase was employed as biocatalyst for the enzymic synthesis of a series of alkyl phenylacetates I (R = H, 4-OH, 4-MeO, 4-NH2, 4-NO2; R1 = Et, Pr) which, based on their mol. similarity to propylparaben, were tested in two acute mice models of seizure (maximal electroshock seizure and s.c. pentylenetetrazol tests). Mol. docking was later applied to explain the observed activities. All the synthesized compounds displayed some degree of protective activity in the maximal electroshock seizure model, whereas none of them showed protection against pentylenetetrazol-induced convulsions. Et 4-methoxyphenylacetate and Pr phenylacetate showed the most promising in vivo results. In consistence with the observed anticonvulsant effects, Pr phenylacetate obtained the best predicted binding energy among the synthesized alkyl phenylacetates.

Latin American Journal of Pharmacy published new progress about Anticonvulsants. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, SDS of cas: 104-01-8.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Zhong, Bingwen published the artcileBinuclear copper iodine cluster-based coordination sheets as photocatalysts for decarboxylative cyanation, HPLC of Formula: 104-01-8, the main research area is copper iodine cluster pyridylbenzene MOF preparation photocatalyst decarboxylative cyanation; crystal structure copper iodine cluster pyridylbenzene coordination sheet.

The authors synthesized two new MOFs (Cu-Tpxa-1 and Cu-Tpxa-2) that were used as heterogeneous photocatalysts, combining photocatalysis and Cu catalysis to achieve decarboxylative radical cyanation reactions. This new heterogeneous catalysis method optimized the redox properties and excited-state lifetimes, providing a new idea for exploring photocatalytic mechanisms.

Chemical Communications (Cambridge, United Kingdom) published new progress about Crystal structure. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, HPLC of Formula: 104-01-8.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Patil, Bhausaheb N. published the artcileTransition metal-catalyzed C-H functionalization of arylacetic acids for the synthesis of benzothiadiazine 1,1-dioxides, Related Products of isoquinoline, the main research area is benzothiadiazine dioxide preparation; aminobenzenesulfonamide arylacetic acid functionalization condensation copper catalyst.

Copper-catalyzed practical route for the synthesis of benzothiadiazine 1,1-dioxides I [R = Ph, 4-FC6H4, 3-ClC6H4, etc.] and II [R1 = Ph, 2-furyl, 2-thienyl, etc.] was developed via C-H functionalization of arylacetic acids to form aromatic aldehydes and their subsequent condensation with 2-aminobenzenesulfonamide. This functional group tolerant approach furnished benzothiadiazine 1,1-dioxide derivatives in good to excellent yields. Broad substrate scope, inexpensive catalyst and high product yields were notable features of this protocol.

Tetrahedron Letters published new progress about Benzothiadiazines Role: SPN (Synthetic Preparation), PREP (Preparation). 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Related Products of isoquinoline.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Kavetsou, Eleni published the artcileNovel 3-aryl-5-substituted-coumarin analogues: Synthesis and bioactivity profile, COA of Formula: C9H10O3, the main research area is phenyl methylcoumarin preparation antioxidant antitumor lipoxygenase inhibition SAR docking; acetyloxy-moiety; coumarins; cytotoxicity; lipoxygenase; molecular modeling; oxyprenylated analogues.

Eighteen 3-phenyl-5-substituted-coumarins, among them six were 5-acetyloxy-derivatives, six 5-hydroxy-derivatives and six 5-geranyloxy-derivatives I [R = hydroxy, acetoxy, geranyloxy; R1 = H, MeO, Br; R2 = H, MeO, Br, O2N, etc.] were synthesized, structurally characterized and their antioxidant activity, lipoxygenase inhibitory ability, as well as their cytotoxic activity against human neuroblastoma SK-N-SH and HeLa adenocarcinoma cell lines were evaluated. The compounds I [R = hydroxy, acetoxy, geranyloxy; R1 = H, MeO, Br; R2 = H, MeO, Br, O2N, etc.] were found to be the best cytotoxic agents among all the compounds studied. The bromo-substituted coumarins I [R = acetoxy, R1 = H, R2 = Br; R = acetoxy, R1 = Br, R2 = H] were remarkably active against HeLa cell line showing IC50 1.8 and 6.1μM, resp. Coumarin I [R = geranyloxy, R1 = MeO, R2 = H] presented dual bioactivity, while compound I [R = geranyloxy, R1 = H, R2 = MeO] was the most competent soybean lipoxygenase inhibitor of this series (IC50 10μM). As shown by in-silico docking studies, the studied mols. present allosteric interactions with soybean lipoxygenases.

Drug Development Research published new progress about Antioxidants. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, COA of Formula: C9H10O3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Li, Qing published the artcileSynthesis of (1,3,4-thiadiazol-2-yl)-acrylamide derivatives as potential antitumor agents against acute leukemia cells, Related Products of isoquinoline, the main research area is thiadiazole acrylamide preparation antitumor leukemia caspase dependent apoptosis; (1,3,4-thiadiazol-2-yl)-acrylamide; Acute leukemia; Antitumor agents; Cell apoptosis; Cytotoxicity.

A lead compound with the (1,3,4-thiadiazol-2-yl)-acrylamide scaffold was discovered to have significant cytotoxicity on several tumor cell lines in an inhouse cell-based screening. A total of 60 derivative compounds were then synthesized and tested in a CCK-8 cell viability assay. Some of them exhibited improved cytotoxic activities. The most potent compounds had IC50 values of 1-5μM on two acute leukemia tumor cell lines, i.e. RS4;11 and HL-60. Flow cytometry anal. of several active compounds and detection of caspase activation indicated that they induced caspase-dependent apoptosis. It was also encouraging to observe that these compounds did not have obvious cytotoxicity on normal cells, i.e. IC50 > 50μM on HEK-293T cells. Although the mol. targets of this class of compound are yet to be revealed, our current results suggest that this class of compound represents a new possibility for developing drug candidates against acute leukemia.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Related Products of isoquinoline.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Luo, Guolin published the artcileDesign, synthesis and antitumor evaluation of novel 5-methylpyrazolo[1,5-a]pyrimidine derivatives as potential c-Met inhibitors, Product Details of C9H10O3, the main research area is methyl pyrazolopyrimidine preparation antitumor cMet kinase inhibitor docking SAR; Antitumor activity; Molecular docking; Pyrazolo[1,5-a]pyrimidine derivatives; Synthesis; c-Met kinase inhibitor.

A series of novel 5-methylpyrazolo[1,5-a]pyrimidine derivatives I (R = pyrazin-2-yl, 4-chlorophenyl, 2-fluorobenzyl, etc.; R1 = H, Me) were designed, synthesized, and evaluated for their in vitro inhibitory activities against c-Met kinase and antiproliferative activities against the SH-SY5Y, MDA-MB-231, A549, and HepG2 cell lines. Most of the compounds remarkably inhibited c-Met kinase and showed moderate to good cytotoxicity and selectivity toward the four cancer cell lines. Among them, compounds I (R = pyrazin-2-yl, 4-fluorophenyl; R1 = H) were the two most potent selective c-Met inhibitors with half-maximal inhibitory concentration (IC50) values of 5.17 ± 0.48 nM and 5.62 ± 0.78 nM, resp., and suppression abilities comparable with the pos. control cabozantinib. Cell proliferation assay further demonstrated that the two most promising compounds I (R = 3,5,6-trimethylpyrazin-2-yl, pyrazin-2-yl, ; R1 = H) also showed good cytotoxicity and selectivity toward MDA-MB-231 cells, with IC50 values of 26.67 ± 2.56μM and 26.83 ± 2.41μM, resp. Compounds I (R = 4-fluorophenyl, 4-methoxy-3-fluorophenyl; R1 = H) showed cytotoxicity and selectivity toward A549 cells, with IC50 values of 20.20 ± 2.04μM and 21.65 ± 1.58μM, resp. All antiproliferative activities were within the range of those of cabozantinib. Notably, these compounds I presented relatively low hepatotoxicity compared with reference drugs. Moreover, the preliminary structure-activity relationship and docking studies revealed that replacement of a nitrogen-containing heterocycle on the R (block A) group might improve the c-Met kinase inhibitory and antiproliferative effects in MDA-MB-231 cells, whereas displacement by a substituted benzene ring, especially for the p-fluorophenyl or 4-fluoro-3-methoxyphenyl moiety, on the R group enhanced cytotoxicity toward A549 cells. Together, these results suggest that I (R = pyrazin-2-yl, 4-fluorophenyl; R1 = H) are promising compounds and provide a basis for their development as new antitumor agents.

Bioorganic Chemistry published new progress about Antitumor agents. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Product Details of C9H10O3.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Liu, Jun published the artcileNovel 2-Substituted 3-Hydroxy-1,6-dimethylpyridin-4(1H)-ones as Dual-Acting Biofilm Inhibitors of Pseudomonas aeruginosa, Application of 4-Methoxyphenylacetic acid, the main research area is hydroxy dimethylpyridinone synthesis drug design Pseudomonas aeruginosa biofilm inhibitor.

2-Heptyl-3-hydroxy-4(1H)-quinolone (PQS), a compound from P. aeruginosa, functions as both a quorum sensing (QS) regulator and a potent iron chelator to induce expression of pyoverdine and pyochelin which are involved in high-affinity iron transport systems. A potential dual-acting antibiofilm strategy requires mols. designed to interfere with iron uptake and the QS system of P. aeruginosa. A series of 2-substituted 3-hydroxy-1,6-dimethylpyridin-4-ones have been designed, synthesized, and tested as biofilm inhibitors of P. aeruginosa. One compound, N-((1,3,6-trimethyl-4-oxo-1,4-dihydropyridin-2-yl)methyl)hexanamide, I, exhibits 68.67% biofilm inhibitory activity at 20μM. Further mechanistic studies have confirmed that this compound not only inhibits the QS systems of P. aeruginosa but also acts as an iron chelator to compete strongly with pyoverdine, causing iron deficiency in bacteria. The pyoverdine receptor FpvA was revealed as the target of I by the Pvds mutant strain, fpvA-overexpressed strain, and in silico studies.

Journal of Medicinal Chemistry published new progress about Antibiotic resistance (bacterial). 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Application of 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Bao, Ming published the artcileGold-Catalyzed 1,2-Acyloxy Migration/Coupling Cascade of Propargyl Diazoacetates: Synthesis of Isomycin Derivatives, Safety of 4-Methoxyphenylacetic acid, the main research area is propargyl diazoacetate gold catalyst carbocyclization acyloxy migration coupling cascade; isomycin derivative preparation.

An efficient gold(I)-catalyzed carbocyclization reaction for the synthesis of isomycin derivatives from propargyl diazoacetates has been developed. The suggested cyclization pathway delineated the first example of a vinyl gold carbenoid species generated in situ from gold(I)-catalyzed 1,2-acyloxy migration and intercepted by a cross-coupling reaction with the remaining tethered diazo functionality. The use of protic additives was essential to regulating the reaction outcome by fine-tuning the catalytic preference of the gold(I) complex.

Organic Letters published new progress about Cross-coupling reaction. 104-01-8 belongs to class isoquinoline, name is 4-Methoxyphenylacetic acid, and the molecular formula is C9H10O3, Safety of 4-Methoxyphenylacetic acid.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem