Month: November 2022

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

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

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

Holmberg-Douglas, Natalie published the artcileArene Cyanation via Cation-Radical Accelerated-Nucleophilic Aromatic Substitution, Recommanded Product: 1,3-Dimethoxybenzene, the main research area is aryl nitrile chemoselective preparation; acridinium catalyst photochem nucleophilic aromatic substitution aryl alkyl ether; chemoselective photochem cyanation aryl alkyl ether acetone cyanohydrin; calculation atomic charge radical cation regioselectivity photochem cyanation.

In the presence of a highly oxidizing acridinium tetrafluoroborate, aryl Me ethers and an aryl benzyl ether underwent chemoselective nucleophilic aromatic substitution reactions with cyanide generated in situ from acetone cyanohydrin and NaHCO3 in 1,2-dichloroethane/2,2,2-trifluoroethanol to yield aryl nitriles. The observed selectivities for nucleophilic aromatic substitution over direct cyanation correlated with the sites with the largest increases in pos. charge between the ethers and their radical cations; the transition state structures and activation barriers for cyanation of veratrole and Me 3,4-dimethoxybenzoate and cyanation kinetics and lack of linear free energy relationships were determined

Organic Letters published new progress about Aromatic nitriles Role: PEP (Physical, Engineering or Chemical Process), RCT (Reactant), SPN (Synthetic Preparation), PROC (Process), RACT (Reactant or Reagent), PREP (Preparation). 151-10-0 belongs to class isoquinoline, name is 1,3-Dimethoxybenzene, and the molecular formula is C8H10O2, Recommanded Product: 1,3-Dimethoxybenzene.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Hou, Yanxia published the artcileA novel detection strategy for odorant molecules based on controlled bioengineering of rat olfactory receptor I7, Recommanded Product: 2-Methyl-3-(3,4-methylenedioxyphenyl)propionaldehyde, the main research area is odorant detection bioengineering olfactory receptor immobilization selfassembly biosensor.

In this study, we report a dose-dependent detection of odorant mols. in solution by rat olfactory receptor I7 (OR I7) in its membrane fraction. The OR I7 is immobilized on a gold electrode by multilayer bioengineering based on a mixed self-assembled monolayer and biotin/avidin system, which allows for a well-controlled immobilization of the bioreceptor within its lipid environment. The odorant detection is electronically performed in a quant. manner by electrochem. impedance spectroscopy (EIS) measurements on samples and controls.

Biosensors & Bioelectronics published new progress about Avidins Role: PEP (Physical, Engineering or Chemical Process), TEM (Technical or Engineered Material Use), PROC (Process), USES (Uses). 1205-17-0 belongs to class isoquinoline, name is 2-Methyl-3-(3,4-methylenedioxyphenyl)propionaldehyde, and the molecular formula is C11H12O3, Recommanded Product: 2-Methyl-3-(3,4-methylenedioxyphenyl)propionaldehyde.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Singh, Manvendra published the artcileBroad assessment of bioactivity of a collection of spiroindane pyrrolidines through “”cell painting””, Formula: C9H10O3, the main research area is spiroindane pyrrolidine bioactivity cell painting; Biological activity; Complexity; Fingerprints; Photochemistry.

A collection of small mols. has been synthesized by composing photo-cycloaddition, C-H functionalization, and N-capping strategies. Multidimensional biol. fingerprints of mols. comprising this collection have been recorded as changes in cell and organelle morphol. This untargeted, phenotypic approach allowed for a broad assessment of biol. activity to be determined Reproducibility and the magnitude of measured fingerprints revealed activity of several treatments. Reactive functional groups, such as imines, dominated the observed activity. Two non-reactive candidate compounds with distinct bioactivity fingerprints were identified, as well.

Bioorganic & Medicinal Chemistry published new progress about Carbamoylation (capping reaction). 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, Formula: C9H10O3.

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

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

Wang, Jiaqin published the artcileInvestigation of Deep Eutectic Solvent-Based Microwave-Assisted Extraction and Efficient Recovery of Natural Products, Application of 1-Methylurea, the main research area is deep eutectic solvent microwave assisted natural.

A systematic study of the principles of deep eutectic solvent microwave-assisted extraction (DES-MAE) was performed. It was found that the heating rates of most DESs decreased (heat capacity increased) under microwave irradiation with increasing water content, allowing high-efficiency extraction for thermally sensitive compounds In addition, DESs containing carboxylic acids reacted with hydroxyl groups of sugar and choline chloride, resulting in cell wall destruction and inhibition of cellulose, hemicellulose and lignin reconnection in cell walls through hydrogen bonds, thus leading to better extraction performance. This was verified by extracting anthraquinones from rheum palmatum by using DES-MAE and optimizing extraction conditions. DES with citric acid as the hydrogen bonding donor gave the highest extraction efficiency under the optimized conditions. In addition, anthraquinones in the DES extract were recovered by using three kinds of silica modified by different functional groups. The results showed that material containing a Ph group is beneficial to the recovery of anthraquinones in acid-based DESs, because it can facilitate strong hydrophobic and π-π interactions. This study showcased the green chem. applications of DES-MAE in laboratory and industrial alike, and demonstrates the recovery of natural products from DES extracts The findings also provide valuable information for green extraction, modification, and applications of cellulose, hemicellulose and lignin.

ACS Sustainable Chemistry & Engineering published new progress about Biomass. 598-50-5 belongs to class isoquinoline, name is 1-Methylurea, and the molecular formula is C2H6N2O, Application of 1-Methylurea.

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem