Day: April 2, 2021

Synthetic Route of 63675-74-1, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 63675-74-1, 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene, introducing its new discovery.

Discovery of LSZ102, a potent, orally bioavailable selective estrogen receptor degrader (SERD) for the treatment of estrogen receptor positive breast cancer

In breast cancer, estrogen receptor alpha (ERalpha) positive cancer accounts for approximately 74% of all diagnoses, and in these settings, it is a primary driver of cell proliferation. Treatment of ERalpha positive breast cancer has long relied on endocrine therapies such as selective estrogen receptor modulators, aromatase inhibitors, and selective estrogen receptor degraders (SERDs). The steroid-based anti-estrogen fulvestrant (5), the only approved SERD, is effective in patients who have not previously been treated with endocrine therapy as well as in patients who have progressed after receiving other endocrine therapies. Its efficacy, however, may be limited due to its poor physicochemical properties. We describe the design and synthesis of a series of potent benzothiophene-containing compounds that exhibit oral bioavailability and preclinical activity as SERDs. This article culminates in the identification of LSZ102 (10), a compound in clinical development for the treatment of ERalpha positive breast cancer.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Synthetic Route of 63675-74-1. In my other articles, you can also check out more blogs about 63675-74-1

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

 

Electric Literature of 22913-24-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.22913-24-2, Name is Methyl benzo[b]thiophene-2-carboxylate, molecular formula is C10H8O2S. In a Article£¬once mentioned of 22913-24-2

A New Indirect Application of Aggregative Activation: Synthesis of Esters by Cobalt-Catalyzed Carbonylation of Aryl, Heterocyclic, and Vinyl Halides under Atmospheric Pressure

Sun lamp illuminated alkoxycarbonylation of aryl, heteroaryl, and vinyl halides was performed under atmospheric pressure of CO in the presence of a cobalt catalyst in situ generated from Co(OAc)2.Illunination through a Pyrex flask was sufficient to catalyze the reaction.This process avoids the use of Co2(CO)8 and excess CH3I, which were required in the earlier procedure.A SRN1 mechanism is proposed.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 22913-24-2, and how the biochemistry of the body works.Electric Literature of 22913-24-2

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

 

Synthetic Route of 63675-74-1, 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. 63675-74-1, Name is 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene, molecular formula is C16H14O2S. In a Article£¬once mentioned of 63675-74-1

Discovery and synthesis of [6-hydroxy-3-[4-[2-(1- piperidinyl)ethoxy]phenoxy]-2-(4-hydroxyphenyl)]benzo[b]thiophene: A novel, highly potent, selective estrogen receptor modulator

Raloxifene,[2-(4-hydroxyphenyl)-6-hydroxybenzo[b]thien-3-yl][4-[2-(1- piperidinyl)ethoxy]phenyl]-methanone hydrochloride (2), is representative of a class of compounds known as selective estrogen receptor modulators (SERMs) that possess estrogen agonist-like actions on bone tissues and serum lipids while displaying potent estrogen antagonist properties in the breast and uterus. As part of ongoing SAR studies with raloxifene, we found that replacement of the carbonyl group with oxygen ([6-hydroxy-3-[4-[2-(1- piperidinyl)ethoxy]phenoxy]-2-(4-hydroxyphenyl)]benzo[b]thiophene hydrochloride, 4c) resulted in a substantial (10-fold) increase in estrogen antagonist potency relative to raloxifene in an in vitro estrogen dependent cell proliferation assay (IC50 = 0.05 nM) in which human breast cancer cells (MCF-7) were utilized. In vivo, 4c potently inhibited the uterine proliferative response to exogenous estrogen in immature rats following both sc and oral dosing (ED50 of 0.006 and 0.25 mg/kg, respectively). In ovariectomized aged rats, 4c produced a significant maximal decrease (45%) in total cholesterol at 1.0 mg/kg (po) and showed a protective effect on bone relative to controls with maximal efficacy at 1.0 mg/kg (po). These data identify 4c as a novel SERM with greater potency to antagonize estrogen in uterine tissue and in human mammary cancer cells compared to raloxifene, tamoxifen or ICI-182,780.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Synthetic Route of 63675-74-1. In my other articles, you can also check out more blogs about 63675-74-1

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

 

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. category: benzothiophene. Introducing a new discovery about 20699-85-8, Name is Methyl 5-aminobenzo[b]thiophene-2-carboxylate

Benzoyl and cinnamoyl nitrogen mustard derivatives of benzoheterocyclic analogues of the tallimustine: Synthesis and antitumour activity

A series of benzoyl and cinnamoyl nitrogen mustards tethered to different benzoheterocycles and to oligopyrroles structurally related to netropsin consisting of two pyrrole-amide units and terminating with an amidine moiety have been synthesised and a structure-activity relationship determined. Derivatives 3-10 have been evaluated for their sequence selective alkylating properties and cytotoxicity against human K562 leukaemia cells. They are 2- to 50-fold less cytotoxic than tallimustine, with compound 8 being the most potent member of this series. Among tallimustine isosters, the compounds with an indole 3 or benzothiophene 6 are 4-fold less cytotoxic than tallimustine, while the compounds with an N-methyl indole or benzofuran showed a 7- and 14-fold reduced cytotoxic potency, respectively. Our preliminary results indicate that these derivatives preferentially bind to AT-rich sequence with a sequence selectivity similar to tallimustine.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Reference of 20532-28-9, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 20532-28-9, Name is 5-Aminobenzothiophene,introducing its new discovery.

Synthesis and SAR studies of bicyclic amine series GPR119 agonists

We disclosed a novel series of G-protein coupled receptor 119 (GPR119) agonists based on a bicyclic amine scaffold. Through the optimization of hit compound 1, we discovered that the basic nitrogen atom of bicyclic amine played an important role in GPR119 agonist activity expression and that an indanone in various bicyclic rings was suitable in this series of compounds. The indanone derivative 2 showed the effect of plasma glucose control in oGTT and scGTT in the rodent model.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 20532-28-9, and how the biochemistry of the body works.Reference of 20532-28-9

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

 

6287-82-7, In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 6287-82-7, name is 2,3-Dibromobenzo[b]thiophene, introducing its new discovery.

BENZOTHIOPHENE DERIVATIVES AND ORGANIC ELECTROLUMINESCENT DEVICES USING THE SAME

The present invention relates to a compound represented by following general formula (I): wherein R1 and R2 are independently selected from a substituted or unsubstituted C4 to C30 arylamine group, a substituted or unsubstituted C4 to C40 carbazole group, a substituted or unsubstituted C4 to C40 benzothiophene group or a substituted or unsubstituted C4 to C40 benzofuran group; L is a bridging group, and selected from a single bond substituted C4 to C40 arylamine group, a substituted C4 to C40 carbazole group, a substituted C4 to C40 benzothiophene group, O atom, N atom or S atom; R3-R10 are independently selected from H atom, a C1-C20 aliphatic compound containing linear or branched alkanes, alkenes or alkynes or a C6-C30 aromatic group, or two adjacent groups linking to be a ring forming a naphthothiophene derivatives; m and n are selected from integers of 1 to 3, as well as the addition of m and n is larger than 0 but less than or equal to 3. Also, the present invention relates to organic electroluminescent devices using the compound represented by general formula (I), especially a hole transporting material, a hole injecting material or a main material of organic luminescent material used in an OLED device.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.6287-82-7, you can also check out more blogs about6287-82-7

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

 

Reference of 1198-51-2, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 1198-51-2, 3-(Bromomethyl)-5-chlorobenzo[b]thiophene, introducing its new discovery.

ANTIDIABETIC COMPOUNDS

Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Reference of 1198-51-2. In my other articles, you can also check out more blogs about 1198-51-2

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

 

Reference of 360575-29-7, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 360575-29-7, Methyl 4-bromobenzo[b]thiophene-2-carboxylate, introducing its new discovery.

Structure-activity relationship study of novel NR2B-selective antagonists with arylamides to avoid reactive metabolites formation

A novel potent NMDA-NR2B selective antagonist (5b) without the reactive metabolites formation issue was identified. Through this study, a close correlation between reactive metabolites formation and calculated HOMO energies of parent compounds was found.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Reference of 360575-29-7. In my other articles, you can also check out more blogs about 360575-29-7

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

 

Chemistry is traditionally divided into organic and inorganic chemistry. HPLC of Formula: C8H5BrS, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 4923-87-9

N-Arylation of Carbamates through Photosensitized Nickel Catalysis

A highly efficient method of visible light mediated Ni(II)-catalyzed photoredox N-arylation of Cbz-amines/Boc-amines with aryl electrophiles at room temperature is reported. The methodology provides a common access to a wide variety of N-aromatic and N-heteroaromatic carbamate products that find use in the synthesis of several biologically active molecules and provides a distinct advantage over traditional palladium-catalyzed Buchwald reaction.

If you are interested in 4923-87-9, you can contact me at any time and look forward to more communication. HPLC of Formula: C8H5BrS

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

 

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

c-MYC G-quadruplex binding by the RNA polymerase I inhibitor BMH-21 and analogues revealed by a combined NMR and biochemical Approach

Background Pyridoquinazolinecarboxamides have been reported as RNA polymerase I inhibitors and represent a novel class of potential antitumor agents. BMH-21, was reported to intercalate with GC-rich rDNA, resulting in nucleolar stress as a primary mechanism of cytotoxicity. Methods The interaction of BMH-21 and analogues with DNA G-quadruplex structures was studied by NMR and molecular modelling. The cellular response was investigated in a panel of human tumor cell lines and protein expression was examined by Western Blot analysis. Results and conclusions We explored the ability of BMH-21 and its analogue 2 to bind to G-quadruplex present in the c-MYC promoter, by NMR and molecular modelling studies. We provide evidence that both compounds are not typical DNA intercalators but are effective binders of the tested G-quadruplex. The interaction with c-MYC G-quadruplex was reflected in down-regulation of c-Myc expression in human tumor cells. The inhibitory effect was almost complete in lymphoma cells SUDHL4 characterized by overexpression of c-Myc protein. This downregulation reflected an early and persistent modulation of cMyc mRNA. Given the relevance of c-MYC in regulation of ribosome biogenesis, it is conceivable that the inhibition of c-MYC contributes to the perturbation of nuclear functions and RNA polymerase I activity. Similar experiments with CX-5461, another RNA polymerase I transcription inhibitor, indicate the same behaviour in G-quadruplex stabilization. General significance Our results support the hypothesis that BMH-21 and analogue compounds share the same mechanism, i.e. G-quadruplex binding as a primary event of a cascade leading to inhibition of RNA polymerase I and apoptosis.

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.Reference of 35212-85-2

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