Category: 1468-83-3

Liang, Jinghui published the artcileDesign and development of novel fasudil derivatives as potent antibreast cancer agent that improves intestinal flora and intestinal barrier function in rats, Application In Synthesis of 1468-83-3, the main research area is breast cancer fasudil invasion microbiota migration ROCK; ROCK; breast cancer; fasudil; invasion; microbiota; migration.

This study was conducted to develop novel fasudil derivatives after incorporation of substituted thiazoles as potent anti-breast cancer (BC) agents. The compounds were developed using a facile synthetic route in excellent yields. The entire set of developed compounds was tested for inhibitory activity against rho-associated coiled-coil kinase (ROCK; ROCK1 and ROCK2) kinase, where they exhibit potent and selective inhibition of ROCK1 as compared to ROCK2. The most potent ROCK2 inhibitor, compound 6h significantly inhibited the viability of BC cells (MCF-7). It also causes inhibition of migration and invasion of MCF-7 cells. Moreover, the anti-BC activity of compound 6h was studied in 7,12 di-Me Benz(a)anthracene (DMBA)-induced BC in female Sprague Dawley rats. Results suggest that it causes significant improvement in the bodyweight of the animals with a reduction in oxidative stress in the liver and mammary tissues of rats. It showed improvement in the intestinal barrier function of rats by restoring the level of Diamine oxidase, D-lactate, and endotoxin. In western blot anal., it showed improvement in (ZO-1), occludin, and claudin-1 in the colon tissue of the rat as compared to the DMBA group. Our study demonstrated the development of the novel class of fasudil derivatives potent anti-BC agent that improves intestinal flora and intestinal barrier function in rats.

Chemical Biology & Drug Design published new progress about Antitumor agents. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Application In Synthesis of 1468-83-3.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Aslam, Sana published the artcileAnticancer activity of structural hybrids of various 5/6-memberedheterocycles with pyrazolobenzothiazine 5,5-dioxide, Category: benzothiophene, the main research area is human gastric liver colon carcinoma memberedheterocycle pyrazolobenzothiazine dioxide anticancer.

Thiophene, furan, coumarin and pyrazolobenzothiazine are well familiar for their biol. activities. In this research, pyrazolobenzothiazine ring system is hybridized with various S, N & O-containing heterocycles and the resulting compounds were screened for their anticancer activity against six different cancer cell lines i.e., KB (human oral carcinoma cells), MCF-7(human breast carcinoma cells), A549 (human alveolar adenocarcinoma cells), Hep-G2 (liver carcinoma cells), SGC-7901(human gastric carcinoma cells) and S1 (human colon carcinoma cells) using MTT assay. Most of the compounds exhibited good activity against KB, S1 and A549 cancer cell lines. 5k and 5p appeared as potent inhibitors of KB cell line with IC50 values 2.78 and 4.39 μM resp., 5q was a potent inhibitor of MCF-7 (IC50 value = 13.64 μM) and 5j an excellent inhibitor of A549 cell line having IC50value of 1.03 μM. 5p and 5q were inhibitors of S1 cell line (IC50 values of 8.29 μM and 7.69 μM resp.), whereas, 5o and 5q as inhibitors of Hep-G2 cell line were discovered. A number of compounds show activity exceeding that of 5-fluoruracil in different cell assays. The most potently active compounds, 5j, 5p and 5q, exhibited selectivity in targeting cancerous cells as compared to normal human PBM cells while, 5k and 5o displayed significant toxicity in normal cells.

Pakistan Journal of Pharmaceutical Sciences published new progress about Antitumor agents. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Category: benzothiophene.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Cao, Hao-Qiang published the artcileDirect Enamido C(sp2)-H Diphosphorylation Enabled by a PCET-Triggered Double Radical Relay: Access to gem-Bisphosphonates, SDS of cas: 1468-83-3, the main research area is amide unsaturated vinylamide oxidative phosphonylation preparation gem diphosphonate; proton coupled electron transfer enamide phosphonylation radical relay process; unsaturated gem vinylidenediphosphonate amino preparation diphosphonylation enamide silver promoted; bisphosphonates; enamides; radical relay; silver; synthetic methods.

Gem-Diphosphonates ArC(NHCOMe):C[P(O)(OR)2]2 (Ar = substituted Ph, pyridyl, pyrrolyl, thienyl, thiazolyl) were prepared by Ag2O-promoted oxidative diphosphonylation of vinylamides CH2:CArNHCOMe with hydrophosphonates HP(O)(OR)2. Herein we report a novel and straightforward protocol for the construction of valuable gem-BPs by means of proton-coupled electron-transfer (PCET)-triggered enamido C(sp2)-H diphosphorylation. This reaction represents a rare example of realizing the challenging double C-P bond formation at a single carbon atom, thus providing facile access to a broad variety of structurally diverse bisphosphonates from simple enamides under silver-mediated conditions. Initial mechanistic studies demonstrated that the diphosphorylation involves two rounds of PCET-initiated radical relay process.

Chemistry – A European Journal published new progress about C-P bond formation. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, SDS of cas: 1468-83-3.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Battula, Satyanarayana published the artcileAccessing Grignard Reluctant Aldehyde in 2-Oxoaldehyde by Organocuprates to Give [1,2] Addition and Oxidative Coupling Reactions, Synthetic Route of 1468-83-3, the main research area is dione preparation; oxoaldehyde preparation Grignard reagent addition and oxidative coupling reaction; ketone hydrolysis.

Novel finding of aldehyde in 2-oxoaldehyde (2OA) is presented as it unprecedentedly disinclines to react with Grignard reagents but reacts with moderate organocuprate reagents in anaerobic condition to give [1,2] addition (α-hydroxyketones) reaction. In the presence of air, the reaction produces an efficient protocol for the synthesis of 1,2-diones through a copper-catalyzed oxidative cross-coupling reaction at room temperature Mechanistic studies indicate that α-hydroxy ketone perhaps is generated before the hydrolysis step/acid work-up process. The α-keto group of 2OA causes to exhibit this peculiar aldehyde behavior toward these organometallic reagents.

ACS Omega published new progress about Addition reaction. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Synthetic Route of 1468-83-3.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Celebioglu, Hasan Ufuk published the artcileCytotoxic effects, carbonic anhydrase isoenzymes, α-glycosidase and acetylcholinesterase inhibitory properties, and molecular docking studies of heteroatom-containing sulfonyl hydrazone derivatives, Computed Properties of 1468-83-3, the main research area is sulfonylhydrazone antitumor carbonic anhydrase glycosidase acetylcholinesterase inhibition mol docking; Heteroatom; antibacterial; anticancer; docking; enzyme inhibition; sulfonyl hydrazone.

Today, interest in studies on the search for new drugs to be used in diseases such as cancer, cardiovascular diseases, neurodegenerative diseases and diabetes, as well as prevention of microbial inflammation is increasing day by day. Emerging biol. and pharmacol. effects of sulfonyl hydrazone derivative compounds reveal their importance. In the present study, heteroatom-containing sulfonyl hydrazone derivatives have been studied for their anticancer and antimicrobial properties, as well as their effects on enzymes that could play roles in Alzheimer′s disease and diabetes. High doses of the tested compounds significantly decreased the cell viabilities of breast cancer (MCF-7) and prostate cancer (PC-3) cell lines. Furthermore, all compounds possessed antimicrobial activities against very common bacteria E. coli and S. aureus. These compounds were good inhibitors of the α-glycosidase, human carbonic anhydrase I and II isoforms and acetylcholinesterase enzyme with Ki values in the range of 1.14 ± 0.14-3.63 ± 0.26 nM for α-glycosidase, 66.05 ± 9.21-125.45 ± 11.54 nM for hCA I, 89.14 ± 10.43-170.22 ± 26.05 nM for hCA II and 754.03 ± 73.22-943.92 ± 58.15 nM for AChE, resp. Mol. docking method was used to theor. compare biol. activities of sulfonyl hydrazone derivatives against enzymes. The theor. results were compared with the exptl. results. Thus, these compounds have strong biol. activities.

Journal of Biomolecular Structure and Dynamics published new progress about Alzheimer disease. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Computed Properties of 1468-83-3.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Secci, Daniela published the artcile4-(3-Nitrophenyl)thiazol-2-ylhydrazone derivatives as antioxidants and selective hMAO-B inhibitors: synthesis, biological activity and computational analysis, Category: benzothiophene, the main research area is nitrophenylthiazolyl hydrazone synthesis antioxidant monoamine oxidase neurodegenerative disorder; (Thiazol-2-yl)hydrazone derivatives; Alzheimer’s disease; Parkinson’s disease; antioxidants; inhibitor; molecular modelling; monoamine oxidase; selective.

A new series of 4-(3-nitrophenyl)thiazol-2-ylhydrazone derivatives were designed, synthesized, and evaluated to assess their inhibitory effect on the human monoamine oxidase (hMAO) A and B isoforms. Different (un)substituted (hetero)aromatic substituents were linked to N1 of the hydrazone in order to establish robust structure-activity relationships. The results of the biol. testing demonstrated that the presence of the hydrazothiazole nucleus bearing at C4 a Ph ring functionalised at the meta position with a nitro group represents an important pharmacophoric feature to obtain selective and reversible human MAO-B inhibition for the treatment of neurodegenerative disorders. In addition, the most potent and selective MAO-B inhibitors were evaluated in silico as potential cholinesterase (AChE/BuChE) inhibitors and in vitro for antioxidant activities. The results obtained from mol. modeling studies provided insight into the multiple interactions and structural requirements for the reported MAO inhibitory properties.

Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Alzheimer disease. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Category: benzothiophene.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Naidek, Naiane published the artcileAnchoring conductive polymeric monomers on single-walled carbon nanotubes: towards covalently linked nanocomposites, Recommanded Product: 3-Acetylthiophene, the main research area is anchoring conductive polymeric monomer walled carbon nanotube covalently nanocomposite.

The functionalization of carbon nanotubes (CNTs) has long been a challenge due to the low reactivity of CNTs. Herein we present a novel approach to covalently functionalize CNTs directly on the carbon surface with three different monomers of conductive polymers. A covalently linked polymeric nanocomposite derived from polypyrrole was also obtained. Highly reactive single-walled carbon nanotube (SWCNT) salts were functionalized with the monomers: 3-bromothiophene, 3-acetylthiophene and 1-(2-bromoethyl)-1H-pyrrole. After the functionalization, a “”grafted from”” approach was used to polymerize the pyrrole-derived SWCNTs and obtain a covalently linked polymeric nanocomposite. All samples were characterized by XPS, thermogravimetric anal., SEM, and IR and Raman spectroscopy. Overall, the results evidence the efficiency of the covalent functionalization directly on the skeleton of the SWCNTs, followed by the polymerization and formation of a novel covalently linked nanocomposite. These materials can benefit future optimal applications such as supercapacitors and artificial muscles.

New Journal of Chemistry published new progress about Artificial muscle. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Recommanded Product: 3-Acetylthiophene.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Rastogi, Gaurav K. published the artcileCu(I)/Fe(III) promoted dicarbonylation of aminopyrazole via oxidative C-H coupling with methyl ketones, COA of Formula: C6H6OS, the main research area is aminopyrazole methyl ketone copper iron dicarbonylation oxidative coupling catalyst; diketone aminopyrazole preparation.

Cu(I)/Fe(III) promoted C4-dicarbonylation of 5-aminopyrazole is developed. The strategy involved radical triggered direct oxidative coupling of 5-aminopyrazoles with Me ketones using aerial oxygen as a source of oxygen in newly generated carbonyl group. CuI is used as catalyst and FeCl3·6H2O is used as additive and the reaction proceeded at 120 °C in DMSO for 9-12 h. It is found that use of Cu(II) catalyst gives the thiomethylated product by reacting with DMSO instead of oxidative coupling. A plausible mechanism is also given.

Tetrahedron Letters published new progress about C-H bond activation. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, COA of Formula: C6H6OS.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Chen, Jinjin published the artcileTransition-metal-free selective pyrimidines and pyridines formation from aromatic ketones, aldehydes and ammonium salts, Category: benzothiophene, the main research area is aryl methylketone arylaldehyde ammonium acetate sodium periodate tandem multicomponent; triarylpyrimidine preparation; acetophenone benzaldehyde ammonium iodide three component cyclocondensaton; triphenylpyridine preparation.

An efficient synthesis of pyrimidines and pyridines was developed from readily available aromatic ketones, aldehydes and ammonium salts under transition-metal-free conditions. In this strategy, ammonium salts were used as nitrogen sources and only water was generated as a nontoxic byproduct. A catalytic amount of NaIO4 played an important role in the selectivity control, whereas substituted pyridines were dominantly formed in its absence.

Green Chemistry published new progress about Aldol condensation. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Category: benzothiophene.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Mahajan, Akhil published the artcileGreen synthesis of silver nanoparticles using green alga (Chlorella vulgaris) and its application for synthesis of quinolines derivatives, Product Details of C6H6OS, the main research area is silver nanoparticle catalyst green alga quinoline derivative.

Nanoparticles were used century ago but have regained their importance in recent years being simple, ecofriendly, pollutant free, nontoxic, low-cost approach, and due good atom economy. The authors demonstrated the synthesis of Ag nanoparticles using green algae (Chlorella vulgaris) which in turn was used for synthesis of biol. important quinolines. Algal extract was prepared and treated with Ag nitrate solution for the synthesis of Ag nanoparticles. Synthesized nanoparticles were characterized with the help of anal. tools like UV, FTIR, x-ray, and SEM and used as a catalyst for the synthesis of quinolines.

Synthetic Communications published new progress about Chlorella vulgaris. 1468-83-3 belongs to class benzothiophene, name is 3-Acetylthiophene, and the molecular formula is C6H6OS, Product Details of C6H6OS.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem