Day: April 12, 2022

Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 122955-13-9, is researched, SMILESS is O=C1C2=C(C=CC=C2)C(CC3=CC=NC=C3)(CC4=CC=NC=C4)C5=CC=CC=C15.[H]Cl.[H]Cl, Molecular C26H22Cl2N2OJournal, Article, Research Support, Non-U.S. Gov’t, British Journal of Pharmacology called Functional brain imaging in larval zebrafish for characterising the effects of seizurogenic compounds acting via a range of pharmacological mechanisms, Author is Winter, Matthew J.; Pinion, Joseph; Tochwin, Anna; Takesono, Aya; Ball, Jonathan S.; Grabowski, Piotr; Metz, Jeremy; Trznadel, Maciej; Tse, Karen; Redfern, Will S.; Hetheridge, Malcolm J.; Goodfellow, Marc; Randall, Andrew D.; Tyler, Charles R., the main research direction is brain imaging larval zebrafish seizurogenic compound CNS safety pharmacol; 3Rs; CNS safety pharmacology; drug discovery/target validation; functional neuroimaging; neuropharmacology; seizures; zebrafish.Recommanded Product: XE991 Dihydrochloride.

Functional brain imaging using genetically encoded Ca2+ sensors in larval zebrafish is being developed for studying seizures and epilepsy as a more ethical alternative to rodent models. Despite this, few data have been generated on pharmacol. mechanisms of action other than GABAA antagonism. Assessing larval responsiveness across multiple mechanisms is vital to test the translational power of this approach, as well as assessing its validity for detecting unwanted drug-induced seizures and testing antiepileptic drug efficacy. Using light-sheet imaging, we systematically analyzed the responsiveness of 4 days post fertilisation (dpf; which are not considered protected under European animal experiment legislation) transgenic larval zebrafish to treatment with 57 compounds spanning more than 12 drug classes with a link to seizure generation in mammals, alongside eight compounds with no such link. We show 4dpf zebrafish are responsive to a wide range of mechanisms implicated in seizure generation, with cerebellar circuitry activated regardless of the initiating pharmacol. Anal. of functional connectivity revealed compounds targeting cholinergic and monoaminergic reuptake, in particular, showed phenotypic consistency broadly mapping onto what is known about neurotransmitter-specific circuitry in the larval zebrafish brain. Many seizure-associated compounds also exhibited altered whole brain functional connectivity compared with controls. This work represents a significant step forward in understanding the translational power of 4dpf larval zebrafish for use in neuropharmacol. studies and for studying the events driving transition from small-scale pharmacol. activation of local circuits, to the large network-wide abnormal synchronous activity associated with seizures.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Catalytic Hydrogenation of Cyclic Carbonates: A Practical Approach from CO2 and Epoxides to Methanol and Diols, published in 2012, which mentions a compound: 1086138-36-4, mainly applied to catalytic hydrogenation cyclic carbonate methanol diol production, Formula: C44H69NP2.

A highly efficient catalytic hydrogenation of cyclic carbonates was developed for the preparation of methanol with the cogeneration of the corresponding diols by using (PNP) Ru”” pincer complexes as the catalysts under relatively mild conditions. This process has provided a facile approach for the simultaneous production of two important bulk chems., methanol and EG, from ethylene carbonate, which is industrially available by reacting ethylene oxide with CO2. The coupling of the present catalytic system with the process of ethylene carbonate production in the omega process is expected to establish a new bridge from CO2 and ethylene oxide to methanol and EG. Apart from the clean production of diol, a big bonus of the present protocol is the efficient chem. utilization of CO2, which represents a distinct advantage in terms of sustainability over the omega process, which gives back CO2. Moreover, this catalytic system has also provided a potential process for the utilization of waste poly(propylene carbonate) as a resource to afford 1,2-propylene diol and methanol through hydrogenative depolymerization, and a convenient method for the preparation of deuterated methanol from CO2 and D2. A possible catalytic mechanism is proposed, in which the NH moiety of the ligand is demonstrated to be critically important in facilitating the reduction of the carbonate C=O bond through secondary coordination sphere interactions with substrates.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: Methyl 3-bromopropanoate, is researched, Molecular C4H7BrO2, CAS is 3395-91-3, about A bright NIR-II fluorescent probe for breast carcinoma imaging and image-guided surgery.Computed Properties of C4H7BrO2.

A novel bright near-IR II (NIR-II, 1000-1700 nm) fluorescent probe with excellent water-solubility, superior photostability, and excellent in vitro and in vivo biocompatibility was facilely synthesized for in vivo biomedical imaging of xenograft breast tumor and chem. induced spontaneous breast carcinoma. To the best of our knowledge, it is the first time that the superior practical applications of this NIR-II probe in dimethylbenzanthracene (DMBA)-induced rat mammary carcinoma imaging and image-guided rat carcinoma surgery were demonstrated.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

HPLC of Formula: 3395-91-3. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: Methyl 3-bromopropanoate, is researched, Molecular C4H7BrO2, CAS is 3395-91-3, about Reductive sp3-sp2 Coupling Reactions Enable Late-Stage Modification of Pharmaceuticals. Author is Mennie, Katrina M.; Vara, Brandon A.; Levi, Samuel M..

Late-stage derivatization of pharmaceutically relevant scaffolds relies on the availability of highly functional-group tolerant reactions. Reactions that increase the sp3 character of mols. enable the pursuit of more selective and well-tolerated pharmaceuticals. Herein, we report the use of sp3-sp2 cross-electrophile reductive couplings to modify a generic ATP-competitive kinase inhibitor with a broad range of primary and secondary alkyl halide coupling partners.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Category: benzothiophene. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: Methyl 3-bromopropanoate, is researched, Molecular C4H7BrO2, CAS is 3395-91-3, about Use of Green Solvents in Metallaphotoredox Cross-Electrophile Coupling Reactions Utilizing Lipophilic Modified Dual Ir/Ni Catalyst System. Author is Delgado, Pete; Glass, Raoul J.; Geraci, Gina; Duvadie, Rohit; Majumdar, Dyuti; Robinson, Richard I.; Elmaarouf, Imran; Mikus, Malte; Tan, Kian L..

Facilitating photoredox coupling reactions in process friendly green solvents was achieved by the successful application of the dual Ir/Ni catalyst system with enhanced solubility properties. These photochem. reactions (specifically Br-Br sp2-sp3 cross electrophile coupling) are reported in a head to head comparison to the reactions using standard di-t-Bu bipyridine ligand Ir/Ni catalyst system. This presentation highlights the benefits of altering the solubility properties of the ligands used in the Ir/Ni dual catalyst.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 3395-91-3, is researched, Molecular C4H7BrO2, about The Synthesis of a Two-Photon Fluorescence Labelling Probe and its Immunochromatographic Strip for Rapid Diagnosis of COVID-19, the main research direction is two photon fluorescence labeling probe immunochromatog strip COVID19 diagnosis.Recommanded Product: 3395-91-3.

A two-photon fluorescence labeling probe (LP) was synthesized, and LP-Ag was obtained by LP labeling the N-protein antigen (Ag) of COVID-19. LP-Ag was made into an immunochromatog. strip. When a blood sample was added to the sample hole of the test card, it would move forward along the nitrocellulose (NC) film. If the sample contained IgM, the IgM bound to LP-Ag and formed an M line with the coated mouse anti-human IgM antibody, giving a pos. response to the presence of IgM of COVID-19. The sensitivity, specificity, and accuracy of the immunochromatog. strip based on the LP was compared with those of the nucleic acid detection method and the colloidal gold method, proving it to be much simpler than the nucleic acid detection method, which can greatly shorten the detection period, and to be much more stable than the colloidal gold method, which can overcome uncertainty. LP-Ag can be used to image lung tissue with COVID-19 by two-photon fluorescence microscopy (TFM).

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Directed Nickel-Catalyzed Diastereoselective Reductive Difunctionalization of Alkenyl Amines, published in 2021-11-05, which mentions a compound: 3395-91-3, Name is Methyl 3-bromopropanoate, Molecular C4H7BrO2, SDS of cas: 3395-91-3.

We report herein an intermol. syn-arylalkylation and alkenylalkylation of alkenyl amines with two different organohalides (iodides and bromides) using Ni(II) catalyst. The cleavable bidentate quinolinamide was utilized after extensive directing group screening to enable olefin difunctionalization with high levels of regio-, chemo-, and diastereocontrol. This general and practical protocol was compatible with α- or β-substituted terminal alkenes and internal alkenes, providing rapid access to branched aliphatic amines bearing two skipped and vicinal stereocenters with high diastereoselectivities that would otherwise be difficult to synthesize.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: Methyl 3-bromopropanoate( cas:3395-91-3 ) is researched.COA of Formula: C4H7BrO2.Pantelic, Nebojsa D.; Bozic, Bojan; Zmejkovski, Bojana B.; Banjac, Nebojsa R.; Dojcinovic, Biljana; Wessjohann, Ludger A.; Kaluderovic, Goran N. published the article 《In vitro evaluation of antiproliferative properties of novel organotin(IV) carboxylate compounds with propanoic acid derivatives on a panel of human cancer cell lines》 about this compound( cas:3395-91-3 ) in Molecules. Keywords: organotin carboxylate propanoic acid antiproliferative activity cancer cell human; ICP-MS; apoptosis; breast cancer; cytotoxicity; triphenyltin(IV). Let’s learn more about this compound (cas:3395-91-3).

The synthesis of novel triphenyltin(IV) compounds, Ph3SnLn (n = 1-3), with oxaprozin (3-(4,5-diphenyloxazol-2-yl)propanoic acid), HL1, and the new propanoic acid derivatives 3-(4,5-bis(4-methoxylphenyl)oxazol-2-yl)propanoic acid, HL2, and 3-(2,5-dioxo-4,4-diphenylimidazolidin-1-yl)propanoic acid, HL3, has been performed. The ligands represent com. drugs or their derivatives and the tin complexes have been characterized by standard anal. methods. The in vitro antiproliferative activity of both ligands and organotin(IV) compounds has been evaluated on the following tumor cell lines: human prostate cancer (PC-3), human colorectal adenocarcinoma (HT-29), breast cancer (MCF-7), and hepatocellular cancer (HepG2), as well as on normal mouse embryonic fibroblast cells (NIH3T3) with the aid of MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-12 diphenyltetrazolium bromide) and CV (crystal violet) assays. Contrary to the inactive ligand precursors, all organotin(IV) carboxylates showed very good activity with IC50 values ranging from 0.100 to 0.758 μM. According to the CV assay (IC50 = 0.218 ± 0.025 μM), complex Ph3SnL1 demonstrated the highest cytotoxicity against the caspase 3 deficient MCF-7 cell line. Inductively coupled plasma mass spectrometry (ICP-MS) anal. indicated a two-fold lower concentration of tin in MCF-7 cells in comparison to platinum. To investigate the mechanism of action of the compound Ph3SnL1 on MCF-7 cells, morphol., autophagy and cell cycle anal., as well as the activation of caspase and ROS/RNS and NO production, has been performed. Results suggest that Ph3SnL1 induces caspase-independent apoptosis in MCF-7 cells.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: Methyl 3-bromopropanoate( cas:3395-91-3 ) is researched.Quality Control of Methyl 3-bromopropanoate.Cao, Jie; Chi, Jinnan; Xia, Junfei; Zhang, Yanru; Han, Shangcong; Sun, Yong published the article 《Iodinated Cyanine Dyes for Fast Near-Infrared-Guided Deep Tissue Synergistic Phototherapy》 about this compound( cas:3395-91-3 ) in ACS Applied Materials & Interfaces. Keywords: iodinated cyanine dye NIR phototherapy photodynamic therapy; Iodinated cyanine dyes; NIR imaging; enhanced ROS production; photodynamic therapy; photothermal therapy. Let’s learn more about this compound (cas:3395-91-3).

Phototheranostics, which combines deep tissue imaging and phototherapy [photodynamic therapy (PDT) and/or photothermal therapy (PTT)] via light irradiation, is a promising strategy to treat tumors. Near-IR (NIR) cyanine dyes are researched as potential phototheranostics reagents for their excellent photophys. properties. However, the low singlet oxygen generation efficiency of cyanine dyes often leads to inadequate therapeutic efficacy for tumors. Herein, we modified an indocyanine green derivative Cy7 with heavy atom iodine to form a novel NIR dye CyI to improve the reactive oxygen species (ROS) production and heat generation while, at the same time, maintain their fluorescence characteristics for in vivo noninvasive imaging. More importantly, in vitro and in vivo therapeutic results illustrated that CyI could quickly and simultaneously generate enhanced ROS and heat to induce more cancer cell apoptosis and higher inhibition rates in deep HepG2 tumors than other noniodinated NIR dyes upon NIR irradiation Besides, low toxicity of the resulted iodinated NIR dyes was confirmed by in vivo biodistribution and acute toxicity. Results indicate that this low toxic NIR dye could be an ideal phototheranostics agent for deep tumor treatments. Our study presents a novel approach to achieve the fast-synergistic PDT/PTT treatment in deep tissues.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

Product Details of 3395-91-3. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: Methyl 3-bromopropanoate, is researched, Molecular C4H7BrO2, CAS is 3395-91-3, about Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies. Author is Liang, Xuewu; Zang, Jie; Li, Xiaoyang; Tang, Shuai; Huang, Min; Geng, Meiyu; Chou, C. James; Li, Chunpu; Cao, Yichun; Xu, Wenfang; Liu, Hong; Zhang, Yingjie.

Concurrent inhibition of Janus kinase (JAK) and histone deacetylase (HDAC) could potentially improve the efficacy of the HDAC inhibitors in the treatment of cancers and resolve the problem of HDAC inhibitor resistance in some tumors. Here, a novel series of pyrimidin-2-amino-pyrazol hydroxamate derivatives as JAK and HDAC dual inhibitors was designed, synthesized, and evaluated, among which I possessed potent and balanced activities against both JAK2 and HDAC6 with half-maximal inhibitory concentration at the nanomolar level. I exhibited improved antiproliferative and proapoptotic activities over SAHA and ruxolitinib in several hematol. cell lines. Remarkably, I exhibited more potent antiproliferation effect than the combination of SAHA and ruxolitinib in HEL cells bearing JAK2V617F mutation. Pharmacokinetic studies in mice showed that I possessed good bioavailability after i.p. administration. Finally, I showed antitumor efficacy with no significant toxicity in a HEL xenograft model. Collectively, the results confirm the therapeutic potential of JAK and HDAC dual inhibitors in hematol. malignancies and provide valuable leads for further structural optimization and antitumor mechanism study.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem