Month: January 2023

New chemical tools for probing activity and inhibition of the NAD+-dependent lysine deacylase sirtuin 2 was written by Swyter, Soeren;Schiedel, Matthias;Monaldi, Daria;Szunyogh, Sandor;Lehotzky, Attila;Rumpf, Tobias;Ova’di, Judit;Sippl, Wolfgang;Jung, Manfred. And the article was included in Philosophical Transactions of the Royal Society, B: Biological Sciences in 2018.Safety of 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione This article mentions the following:

Sirtuins are NAD+-dependent protein deacylases capable of cleaving off acetyl as well as other acyl groups from the 1-amino group of lysines in histones and other substrate proteins. They have been reported as promising drug targets, and thus modulators of their activity are needed as mol. tools to uncover their biol. function and as potential therapeutics. Here, we present new assay formats that complement existing assays for sirtuin biochem. and cellular target engagement. Firstly, we report the development of a homogeneous fluorescence-based activity assay using unlabeled acylated peptides. Upon deacylation, the free lysine residue reacts with fluorescamine to form a fluorophore. Secondly, using click chem. with a TAMRA-azide on a propargylated sirtuin inhibitor, we prepared the first fluorescently labeled small-mol. inhibitor of Sirt2. This is used in a binding assay, which is based on fluorescence polarization. We used it successfully to map potential inhibitor-binding sites and also to show cellular Sirt2 engagement. By means of these new assays, we were able to identify and characterize novel Sirt2 inhibitors out of a focused library screen. The binding of the identified Sirt2 inhibitors was rationalized by mol. docking studies. These new chem. tools thus can enhance further sirtuin research. In the experiment, the researchers used many compounds, for example, 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9Safety of 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione).

4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9) belongs to benzofurans derivatives. Benzofurans are compounds with a planar structure having 10 pi electrons that include the lone pair on oxygen atom, which makes it more susceptible to electrophilic attack. Introduction of benzofurans in organic synthesis, particularly drug synthesis, involves generally the use of their metalated species as nucleophiles in addition reactions or in metal-catalysed cross-coupling reactions.Safety of 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Condensation of salicylonitrile with some α-halo carbonyl compounds was written by Trofimov, F. A.;Lelyak, G. F.;Shevchenko, L. I.;Grinev, A. N.. And the article was included in Khimiya Geterotsiklicheskikh Soedinenii in 1974.Application of 54802-10-7 This article mentions the following:

Benzofurans (I; R = H, Br, R1 = OMe, NH2, Ph, Me, R2 = Ac, H) were obtained in 20-84% yields by condensation of a salicylonitrile with XCH2COR1 (X = Cl, Br). Hydrolysis of I (R = H, R1 = OMe, R2 = Ac) by NaOH gave 90% I (R = H, R1 = OH, R2 = Ac) which was decarboxylated by heating in DMF to give 31% II. In the experiment, the researchers used many compounds, for example, 3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7Application of 54802-10-7).

3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7) belongs to benzofurans derivatives. Many natural or synthetic compounds containing benzofuran skeletons have been found to possess remarkable activity as agrochemicals and pharmaceuticals. As benzofurans are prone to undergo ring opening of the heterocycle, examples of reduction of this type of aromatics by using dissolving metals are rather scarce.Application of 54802-10-7

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Acidity-triggered TAT-presenting nanocarriers augment tumor retention and nuclear translocation of drugs was written by Jiang, Wei;Wang, Jilong;Yang, Jinbin;He, Zhiwei;Hou, Zhenhui;Luo, Yingli;Wang, Li;Liu, Jing;Zhang, Houbing;Zhao, Yangyang;Zhang, Guoqing;Huang, Fang;Zhou, Xuechang;Yan, Lifeng;Yang, Xianzhu;Wang, Yucai;Wang, Jun. And the article was included in Nano Research in 2018.HPLC of Formula: 38183-12-9 This article mentions the following:

In this work, we demonstrate that a transactivator of transcription (TAT)-presenting nanomedicine (DATAT-NP/Pt), apart from improving tumor accumulation and cellular uptake, can simultaneously enhance tumor retention and promote nuclear translocation of encapsulated platinum prodrugs, and thus improve therapeutic efficacy. Specifically, a protecting 2,3-dimethylmaleic anhydride (DA) corona on the nanomedicine prevented the TAT peptide from serum. DATAT-NP/Pt efficiently accumulated at the tumor site through the enhanced permeability and retention (EPR) effect, followed by acid-triggered TAT presenting within the tumor acidic microenvironment (pH ~6.8). The exposed TAT peptide augmented tumor retention and nuclear translocation of DATAT-NP/Pt. We used a tumor-on-a-chip microfluidic system to real-time mimic and analyze tumor accumulation and retention at physiol. flow conditions and revealed that surface absorption of nanomedicines on tumors was critical in determining their tumor retention and clearance. Furthermore, the TAT peptide rapidly translocated the DATAT-NP/Pt into the perinuclear region, allowing for higher nuclear platinum concentrations and increased Pt-DNA adduct formation in nuclei, which consequently reversed cisplatin resistance. Our work presents a new strategy to overcome pathophysiol. barriers of tumor clearance and insufficient cellular translocation and provides new insights for the design of cancer nanomedicines. In the experiment, the researchers used many compounds, for example, 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9HPLC of Formula: 38183-12-9).

4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9) belongs to benzofurans derivatives. Benzofuran derivatives are one of the most important oxygen-containing heterocycles. They are also prone to polymerisation in the presence of concentrated mineral acids and Lewis acids.HPLC of Formula: 38183-12-9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Synthesis and Evaluation of Antimicrobial Activity of Some Novel Heterocyclic Compounds from 5-Bromosalicylaldehyde was written by Abdel-Aziem, Anhar;Baaiu, Basma S.;Abdelhamid, Abdou O.. And the article was included in Journal of Heterocyclic Chemistry in 2017.Product Details of 38220-75-6 This article mentions the following:

A novel series of coumarins, thiadiazoles, thiazoles, and pyridines were synthesized via reaction of 5-bromosalicylaldehyde with different reagents. Thus, 5-bromosalicylaldehyde was reacted with acetonitrile derivatives affording iminocoumarins, which on hydrolysis with 10% hydrochloric acid, afforded coumarins. On the other hand, reaction of 5-bromosalicylaldehyde with benzylhydrazinecarbodithioate afforded a carbodithioate, which reacted with hydrazonoyl halides, affording 1,3,4-thiadiazoles. Moreover, thiazoles were obtained via reaction of 5-bromosalicylaldehyde with a thiocarbohydrazide derivative and hydrazonoyl halides. However, condensation of 2-acetyl-5-bromobenzofuran with benzaldehyde afforded a chalcone, which reacted with pyridinium bromides to afford pyridine derivatives (I, R = Ph, pMePh, 5-bromobenzofuran-2-yl). Furthermore, pyridines were synthesized from the reaction of a chalcone with different active methylene compounds Reaction of II with ethylchloroacetate, chloroacetone, and chloroacetonitrile afforded thienopyridines (III, Y = CO₂Et, Ac, CN). The structures of the newly synthesized compounds were established based on their spectral data and elemental analyses. Also, selected newly synthesized compounds were screened for their antimicrobial activity against various microorganisms by disk diffusion method. In the experiment, the researchers used many compounds, for example, 1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6Product Details of 38220-75-6).

1-(5-Bromobenzofuran-2-yl)ethanone (cas: 38220-75-6) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. As benzofurans are prone to undergo ring opening of the heterocycle, examples of reduction of this type of aromatics by using dissolving metals are rather scarce.Product Details of 38220-75-6

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

A Cu₉S nanoparticle-based CpG delivery system for synergistic photothermal-, photodynamic- and immunotherapy was written by Zhou, Lulu;Chen, Lv;Hu, Xiaochun;Lu, Yonglin;Liu, Wenjie;Sun, Yanting;Yao, Tianming;Dong, Chunyan;Shi, Shuo. And the article was included in Communications Biology in 2020.Application of 76-54-0 This article mentions the following:

Despite its great potential in cancer therapy, phototherapy, including photothermal therapy (PTT) and photodynamic therapy (PDT), often cause metastasis of tumors. Immunotherapy has revolutionized the cancer treatment owing to the capability of activating immune system to eliminate tumors. However, the integration of phototherapy and immunotherapy in a single nanoagent for cancer therapy is still a challenging task. Here, we fabricated (Cu₉S@mSiO₂-PpIX@MnO₂@CpG (CSPM@CpG)) as a synergistic therapeutic model for phototherapy enhanced immunotherapy. The intracellular uptake of cytosine-phosphate-guanine (CpG) promoted the infiltration of cytotoxic T lymphocytes (CTLs) in tumor tissue, further stimulating the production of interferon gamma (IFN-γ) and remarkably elevating the immune response level. Excellent anti-tumor effects have been achieved by synergistic PTT/PDT/immunotherapy. The metastasis of tumors was effectively inhibited by the immune response of CpG. Thus, our proposed work provides a strategy to combine phototherapy with immunotherapy to enhance the therapeutic efficiency and further inhibit metastasis of tumors. In the experiment, the researchers used many compounds, for example, 2′,7′-Dichloro-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 76-54-0Application of 76-54-0).

2′,7′-Dichloro-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 76-54-0) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. In nature, benzofurans have occupied an important role among the plant phenols & several pharmacologically active compounds.Application of 76-54-0

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Discovery of novel benzofuran scaffold as 4-hydroxyphenylpyruvate dioxygenase inhibitors was written by Huang, Hao;Zhang, Jian-qiu;Liu, Jian-min;Wang, Man-man;Shu, Lei;Yan, Yi-le;Zhan, Xiao-hang;Wang, Ping;Huan, Xue-ting;Zhang, Da-yong. And the article was included in Pest Management Science in 2021.Reference of 1646-27-1 This article mentions the following:

4-Hydroxyphenylpyruvate dioxygenase (HPPD) plays an important role in addressing the issue of plant protection research. This study sheds new light on the differences in mol. scaffold from commercialized HPPD inhibitors. The compounds A1-A18 and B1-B27 were synthesized for in vitro and greenhouse experiments The greenhouse experiment data indicated that compounds B14 and B18 displayed excellent herbicidal activity, which was higher compared to that of mesotrione. In vitro testing indicated that the compounds were HPPD inhibitors. Moreover, mol. simulation results show that the compounds B14, B18, and mesotrione shared similar interplay with surrounding residues, which led to a perfect interaction with the active site of Arabidopsis thaliana HPPD. Based on crop selectivity results, compounds B14 and B18 were selected for maize studies (injury≤10%), indicating its potential for weed control in maize fields. These results showed that the pyrazole-benzofuran structure could be used as possible lead compounds for the development of HPPD inhibitors. In the experiment, the researchers used many compounds, for example, Methyl benzofuran-2-carboxylate (cas: 1646-27-1Reference of 1646-27-1).

Methyl benzofuran-2-carboxylate (cas: 1646-27-1) belongs to benzofurans derivatives.Benzofuran is one of the most significant oxygen-containing heterocycles consisting of fused benzene and furan ring, which are widely presented in various naturally occurring and synthetically active compounds. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antioxidant, antitubercular, antiplasmodial, insecticidal.Reference of 1646-27-1

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Quantification of Free Polyelectrolytes Present in Colloidal Suspension, Revealing a Source of Toxic Responses for Polyelectrolyte-Wrapped Gold Nanoparticles was written by Qiu, Tian A.;Torelli, Marco D.;Vartanian, Ariane M.;Rackstraw, Nathan B.;Buchman, Joseph T.;Jacob, Lisa M.;Murphy, Catherine J.;Hamers, Robert J.;Haynes, Christy L.. And the article was included in Analytical Chemistry (Washington, DC, United States) in 2017.Application of 38183-12-9 This article mentions the following:

Polyelectrolyte (PE) wrapping of colloidal nanoparticles (NPs) is a standard method to control NP surface chem. and charge. As excess polyelectrolytes are usually employed in the surface modification process, it is critical to evaluate different purification strategies to obtain a clean final product and thus avoid ambiguities in the source of effects on biol. systems. In this work, 4-nm-diameter gold nanoparticles (AuNPs) were wrapped with 15 kDa poly(allylamine hydrochloride) (PAH), and three purification strategies were applied: (a) diafiltration or either (b) one round or (c) two rounds of centrifugation. The bacterial toxicity of each of these three PAH-AuNP samples was evaluated for the bacterium Shewanella oneidensis MR-1 and is quant. correlated with the amount of unbound PAH mols. in the AuNP suspensions, as judged by XPS and NMR experiments Dialysis experiments show that for a 15 kDa polyelectrolyte, a 50 kDa dialysis membrane is not sufficient to remove all unbound PAH polymers from a nanoparticle suspension. Together, these data showcase the importance of choosing a proper post-synthesis purification method for polyelectrolyte-wrapped NPs and reveal that apparent toxicity results may be due to unintended free wrapping agents like polyelectrolytes. In the experiment, the researchers used many compounds, for example, 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9Application of 38183-12-9).

4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9) belongs to benzofurans derivatives. Benzofuran derivatives are one of the most important oxygen-containing heterocycles. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antiviral, antimicrobial, antitumor, anti-inflammatory.Application of 38183-12-9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Tandem Synthesis of 2-Carboxybenzofurans via Sequential Cu-Catalyzed C-O Coupling and Mo(CO)₆-Mediated Carbonylation Reactions was written by Mo, Qinliang;Sun, Nan;Jin, Liqun;Hu, Baoxiang;Shen, Zhenlu;Hu, Xinquan. And the article was included in Journal of Organic Chemistry in 2020.Reference of 1646-27-1 This article mentions the following:

A modular tandem synthesis of 2-carboxybenzofurans from 2-gem-dibromovinylphenols has been established based on a sequence of Cu-catalyzed intramol. C-O coupling and Mo(CO)₆-mediated intermol. carbonylation reactions. This protocol allowed one-step access to a broad variety of functionalized benzofuran-2-carboxylic acids, esters, and amides in good to excellent yields under Pd- and CO gas-free conditions. In the experiment, the researchers used many compounds, for example, Methyl benzofuran-2-carboxylate (cas: 1646-27-1Reference of 1646-27-1).

Methyl benzofuran-2-carboxylate (cas: 1646-27-1) belongs to benzofurans derivatives. Benzofuran derivatives have shown many biological activities, including antifungal and antimicrobial properties, and acting as antagonists of H3 receptors and angiotensin II. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antioxidant, antitubercular, antiplasmodial, insecticidal.Reference of 1646-27-1

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Threads for tear film collection and support in quantitative amino acid analysis was written by Avilov, Vitaly;Zeng, Qi;Shippy, Scott A.. And the article was included in Analytical and Bioanalytical Chemistry in 2016.HPLC of Formula: 38183-12-9 This article mentions the following:

The collection of tears for chem. composition anal. is complicated by both the difficulty in sampling the tear film and the relatively low microliter volumes available for anal. The experiments in this study are focused on the demonstration of a method for determining amino acids from tear samples. Phenol red thread was used to absorptively collect tear fluid for qual. and quant. analyses of amino acids in basal, reflex, and emotional tears. The thread is also used as a support for sample preparation followed by elution with a buffer. The phenol red indicator on the thread turns from yellow to red with 15-s tear absorption and allows accurate volume measurement from 100 nL to over 1 μL. Derivatization of amino acids was performed directly on the thread with primary amine reactive fluorescamine for fluorescence detection. Analyte elution was performed via centrifugation with the thread in a pipet tip suspended in a centrifuge tube. Collected tear eluate was analyzed via capillary electrophoresis with LED-induced fluorescence. Glycine, glutamate, and aspartate were baseline resolved and used for method characterization. Recoveries were at 50 % for a single derivation and elution step but average recoveries near 90 % were found with two-step processing. Glutamate and aspartate are shown to be stable stored on thread for 3 days. Basal, reflex, and emotional tears were analyzed from three subjects showing distinct amino acid profiles for each tear type. The demonstration of this method may facilitate the development of routine tear compositional anal. to assess ocular health. [Figure not available: see fulltext.]. In the experiment, the researchers used many compounds, for example, 4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9HPLC of Formula: 38183-12-9).

4-Phenyl-3H,3’H-spiro[furan-2,1′-isobenzofuran]-3,3′-dione (cas: 38183-12-9) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Substituted benzofurans find applications such as fluorescent sensors, oxidants, in drug discovery, and in another field of chemistry and agriculture.HPLC of Formula: 38183-12-9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Ru-catalyzed branched versus linear selective C3-alkylation of 2-aroylbenzofurans with acrylates via C-H activation was written by Kommagalla, Yadagiri;Srinivas, Kolluru;Ramana, Chepuri V.. And the article was included in Chemistry – A European Journal in 2014.COA of Formula: C10H8O3 This article mentions the following:

The carbonyl-directed C3-H activation and alkylation of 2-aroylbenzo[b]furans with acrylates occurs selectively either in a linear or branched fashion, depending on the catalyst employed; [Ru(p-cymene)Cl₂]₂ or Ru(PPh₃)₃Cl₂, resp. Two alternate pathways-funded upon the differences in steric and electronic preferences of these two complexes is proposed for the selectivity of linear vs. branched products. © 2014 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim. In the experiment, the researchers used many compounds, for example, Methyl benzofuran-2-carboxylate (cas: 1646-27-1COA of Formula: C10H8O3).

Methyl benzofuran-2-carboxylate (cas: 1646-27-1) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Benzofurans have also made significant and distinctive contributions to biology. They exhibit several biological activities that range from antiviral, antimicrobial, antitumor, anti-inflammatory.COA of Formula: C10H8O3

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem