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Synthesis and biological evaluation of 2-(alkoxycarbonyl)-3-anilinobenzo[b] thiophenes and thieno[2,3-b]pyridines as new potent anticancer agents

Two new series of inhibitors of tubulin polymerization based on the 2-(alkoxycarbonyl)-3-(3?,4?,5?-trimethoxyanilino)benzo[b] thiophene and thieno[2,3-b]pyridine molecular skeletons were synthesized and evaluated for antiproliferative activity on a panel of cancer cell lines, inhibition of tubulin polymerization, cell cycle effects, and in vivo potency. Antiproliferative activity was strongly dependent on the position of the methyl group on the benzene portion of the benzo[b]thiophene nucleus, with the greatest activity observed when the methyl was located at the C-6 position. Also, in the smaller thieno[2,3-b]pyridine series, the introduction of the methyl group at the C-6 position resulted in improvement of antiproliferative activity to the nanomolar level. The most active compounds (4i and 4n) did not induce cell death in normal human lymphocytes, suggesting that the compounds may be selective against cancer cells. Compound 4i significantly inhibited in vivo the growth of a syngeneic hepatocellular carcinoma in Balb/c mice.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Reference of 35212-85-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.35212-85-2, Name is Methyl 3-aminobenzo[b]thiophene-2-carboxylate, molecular formula is C10H9NO2S. In a Article,once mentioned of 35212-85-2

Synthesis and evaluation of apoptosis induction of thienopyrimidine compounds on KRAS and BRAF mutated colorectal cancer cell lines

Monoclonal antibodies (MoAb) and tyrosine kinase inhibitors (TKI) targeting the EGFR (Epidermal Growth Factor Receptor) pathways are currently used in colorectal cancer treatment. Despite the improvement of median overall survival, resistance is observed notably due to KRAS and BRAF gene mutations. We synthesized four series of thienopyrimidines whose scaffold is structurally close to TKI used in clinical practice. We evaluated apoptosis induced by these compounds using flow cytometry on KRAS and BRAF mutated cell lines. Our results confirm that the mutated cell lines (HCT116 and HT29) are more resistant to apoptosis than the non-mutated cell line (Hela). Interestingly, among the 13 compounds tested, three of them (5b, 6b and 6d) and gefitinib exhibited a noteworthy pro-apoptotic effect, especially on mutated cell lines with an IC50 value between 70 and 110 muM. These three compounds seem particularly attractive for the development of novel treatments for colorectal cancer patients harboring EGFR pathway mutations.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Electric Literature of 35212-85-2, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 35212-85-2, Name is Methyl 3-aminobenzo[b]thiophene-2-carboxylate,introducing its new discovery.

3-ALKYL-4-AMIDO-BICYCLIC [4,5,0] HYDROXAMIC ACIDS AS HDAC INHIBITORS

The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.

We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 35212-85-2, and how the biochemistry of the body works.Electric Literature of 35212-85-2

Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Application In Synthesis of Methyl 3-aminobenzo[b]thiophene-2-carboxylate, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 35212-85-2, in my other articles.

Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. Application In Synthesis of Methyl 3-aminobenzo[b]thiophene-2-carboxylate, In an article, mentioned the application of 35212-85-2, Name is Methyl 3-aminobenzo[b]thiophene-2-carboxylate, molecular formula is C10H9NO2S

COMPOUND AND ORGANIC LIGHT EMITTING DEVICE COMPRISING SAME

The present specification provides a compound represented 1 by chemical formula (I) and an organic light-emitting device including the same. (by machine translation)

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Application In Synthesis of Methyl 3-aminobenzo[b]thiophene-2-carboxylate, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 35212-85-2, in my other articles.

Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 35212-85-2, and how the biochemistry of the body works.Electric Literature of 35212-85-2

Electric Literature of 35212-85-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.35212-85-2, Name is Methyl 3-aminobenzo[b]thiophene-2-carboxylate, molecular formula is C10H9NO2S. In a Article,once mentioned of 35212-85-2

An Aryne-Based Route to Substituted Benzoisothiazoles

The combination of arynes, generated using fluoride from the corresponding 2-(trimethylsilyl)aryl triflates, and 3-hydroxy-4-aminothiadiazoles leads to the selective formation of 3-amino-substituted benzo[d]isothiazoles. Variation of the substitution pattern of the aryne precursor, and of the thiadiazole, is possible, with the target heterocycles being obtained in good to excellent yields. In all cases, use of 3-hydroxy-4-aminothiadiazoles leads to incorporation of the amino-substituent in the product heterocycle.

We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 35212-85-2, and how the biochemistry of the body works.Electric Literature of 35212-85-2

Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Brief introduction of C10H9NO2S

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Electric Literature of 35212-85-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.35212-85-2, Name is Methyl 3-aminobenzo[b]thiophene-2-carboxylate, molecular formula is C10H9NO2S. In a Article£¬once mentioned of 35212-85-2

Benzyl derivatives of 2,1,3-benzo- and benzothieno[3,2-a]thiadiazine 2,2-dioxides: First phosphodiesterase 7 inhibitors

The synthesis of a new family of benzyl derivatives of 2,1,3-benzo- and benzothieno[3,2-a]-thiadiazine 2,2-dioxides was achieved. The biological data revealed the first heterocyclic family of compounds with PDE 7 inhibitory properties appearing to be a new objective for the treatment of T-cell- dependent disorders. The IC50 values or percent inhibition values of the compounds against PDE 7 were calculated by testing them against human recombinant PDE 7 expressed in S. cerevisiae. In this expression system the only cyclic nucleotide hydrolyzing activity present in cell extracts corresponded to human PDE 7. Isoenzyme selectivity PDE 7 versus PDE 4 and PDE 3 was also measured. Considering simultaneously inhibition of the three different isoenzymes, monobenzyl derivatives 15 and 23 showed interesting PDE 7 potency (around 10 muM); although not statistically significant, a trend toward selectivity with respect to PDE 3 and PDE 4 was obtained. Benzothiadiazine 16, although less potent at PDE 7 (IC50 = 25 muM), also showed a trend of selectivity toward PDE 3 and PDE 4. These compounds are considered the best leads for further optimization.

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Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

More research is needed about 35212-85-2

A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 35212-85-2

Application of 35212-85-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.35212-85-2, Name is Methyl 3-aminobenzo[b]thiophene-2-carboxylate, molecular formula is C10H9NO2S. In a Article£¬once mentioned of 35212-85-2

Pyrimido<5,4-b>benzofuran and pyrimido<5,4-b>benzothiophene derivatives. Ligands for alpha1- and 5HT1A-receptors

A number of 3-phenylpiperazinylethyl pyrimido<5,4-b>benzofuran-2,4-dione and pyrimido<5,4-b>benzothiophene-2,4-dione derivatives 5-15 were designed as bioisosters of the previously reported pyrimido<5,4-b>indole-2,4-diones and synthesized starting from the 3-amino-2-carboxybenzofuran and benzothiophene ethyl and methyl esters respectively.They were evaluated for their in vitro alpha1-adrenoceptor and 5HT1A-receptor affinities by radioligand receptor binding assays.All target compounds showed good to excellent affinities for the alpha1-adrenoceptor with Ki values in the subnanomolar range.Some compounds were also good ligands for the 5HT1A-receptor with Ki values in the nanomolar range. 3-<2-<4-(2-Methoxyphenyl)piperazin-1-yl>ethyl>-1-methyl pyrimido<5,4-b>benzothiophen-2,4-dione 15 was the most active derivative in displacing <3H>-8-OH-DPAT from rat hippocampal membranes.There is evidence suggesting that the N1 methyl group of the tricyclic moiety of the title compounds is probably able to undergo a Van der Walls interaction at the 5HT1A-receptor binding site but not at the alpha1-adrenoceptor active site. pyrimido<5,4-b>benzofurans / pyrimido<5,4-b>benzothiophenes / alpha1-adrenoceptor binding / 5HT1A-receptor binding

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Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Properties and Exciting Facts About C10H9NO2S

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Reference of 35212-85-2. In my other articles, you can also check out more blogs about 35212-85-2

Reference of 35212-85-2, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 35212-85-2, Name is Methyl 3-aminobenzo[b]thiophene-2-carboxylate, molecular formula is C10H9NO2S. In a Patent£¬once mentioned of 35212-85-2

Thiazine derivatives

The invention relates to thiazine derivatives of the formula STR1 wherein R1 is lower alkyl and R2 is the residue of an aromatic heterocycle containing 1 to 4 hetero atoms optionally substituted by one or two lower alkyl groups, or a phenyl or benzyl group optionally substituted by halogen, hydroxy, lower alkyl, trifluoromethyl, nitro or lower alkoxy, and pharmaceutically acceptable salts thereof. The compounds of formula I are useful for the control or prevention of inflammation, pains, rheumatics and thromboses.

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Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Extracurricular laboratory:new discovery of Methyl 3-aminobenzo[b]thiophene-2-carboxylate

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, Computed Properties of C10H9NO2S, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 35212-85-2

In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. The reactant in an enzyme-catalyzed reaction is called a substrate. Computed Properties of C10H9NO2S, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 35212-85-2, Name is Methyl 3-aminobenzo[b]thiophene-2-carboxylate, molecular formula is C10H9NO2S

FUSED CYCLIC MODULATORS OF NUCLEAR HORMONE RECEPTOR FUNCTION

Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

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Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels.In a patent£¬Which mentioned a new discovery about 35212-85-2, molcular formula is C10H9NO2S, introducing its new discovery. , 35212-85-2

CONDENSED COMPOUND AND ORGANIC LIGHT EMITTING DEVICE INCLUDING THE SAME

Disclosed is a novel condensed cyclic compound and an organic light emitting device including the same.COPYRIGHT KIPO 2015

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, 35212-85-2, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 35212-85-2

Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem