Heterocyclic Building Block-benzofuran

Decline in forced vital capacity in subjects with systemic sclerosis-associated interstitial lung disease in the SENSCIS trial compared with healthy reference subjects was written by Maher, Toby M.;Bourdin, Arnaud;Volkmann, Elizabeth R.;Vettori, Serena;Distler, Jorg H. W.;Alves, Margarida;Stock, Christian;Distler, Oliver. And the article was included in Respiratory Research in 2022.Recommanded Product: 24280-93-1 This article mentions the following:

The forced vital capacity (FVC) of healthy individuals depends on their age, sex, ethnicity and height. Systemic sclerosis-associated interstitial lung disease (SSc-ILD) is characterized by loss of FVC. We compared FVC values in the subjects with SSc-ILD in the SENSCIS trial of nintedanib vs. placebo with values from hypothetical matched healthy references The SENSCIS trial enrolled subjects with SSc with first non-Raynaud symptom in the prior ≤ 7 years, extent of fibrotic ILD on HRCT ≥ 10%, and FVC ≥ 40% predicted. FVC at baseline and decline in FVC over 52 wk were compared with FVC values in hypothetical healthy reference subjects matched 1:1 to the subjects in the trial for age, sex, ethnicity and height, determined using equations published by the European Respiratory Society Global Lung Function Initiative. At baseline, mean (SD) FVC was 2460 (737) mL in the nintedanib group (n = 287) compared with 3403 (787) mL in the hypothetical matched healthy references Mean (SD) FVC was 2544 (817) mL in the placebo group (n = 286) compared with 3516 (887) mL in the hypothetical matched healthy references Mean (SE) changes in FVC at week 52, i.e., age-related loss of lung function, in the hypothetical healthy references matched to the nintedanib and placebo groups, resp., were – 26.3 (0.5) mL and – 25.8 (0.5) mL. The difference in the change in FVC at week 52 between the nintedanib group and the hypothetical healthy references was 26.6 mL (95% CI: 1.2, 52.0; p = 0.04). The difference in the change in FVC at week 52 between the placebo group and the hypothetical healthy references was 77.5 mL (95% CI: 51.4, 103.7; p < 0.0001). Subjects with SSc-ILD in the SENSCIS trial had impaired lung function at baseline and experienced further deterioration over 52 wk. The decline in FVC in the placebo group was four-fold greater than in a hypothetical group of matched healthy references, whereas the decline in FVC in patients who received nintedanib was two-fold greater than in hypothetical healthy references These data highlight the clin. relevance of the slowing of FVC decline provided by nintedanib. In the experiment, the researchers used many compounds, for example, (E)-6-(4-Hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enoic acid (cas: 24280-93-1Recommanded Product: 24280-93-1).

(E)-6-(4-Hydroxy-6-methoxy-7-methyl-3-oxo-1,3-dihydroisobenzofuran-5-yl)-4-methylhex-4-enoic acid (cas: 24280-93-1) 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.Recommanded Product: 24280-93-1

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Ni₂P nanowire arrays grown on Ni foam as an efficient monolithic cocatalyst for visible light dye-sensitized H₂ evolution was written by Wang, Fang;Liu, Tongliang;Liu, Zhaoting;Zhang, Zhengguo;Min, Shixiong. And the article was included in Dalton Transactions in 2022.Recommanded Product: Sodium 2′,4′,5′,7′-tetraiodo-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-bis(olate) This article mentions the following:

Nanostructured H2 evolution cocatalysts are able to promote charge separation and thus enhance the efficiency of the photocatalytic H2 evolution reaction (HER). However, the nanosized cocatalyst particles are easily detached from the surfaces of semiconductors or severely aggregated in reaction systems, which not only greatly reduces the photocatalytic HER efficiency during long-term use but also greatly increases the difficulty of recovery. Moreover, powdery cocatalysts have poor compatibility with the scale-up photoelectrochem. devices. In this paper, a monolithic cocatalyst is developed by controllably growing Ni2P nanowire arrays on Ni foam substrate (Ni2P NWAs/NF) via a direct vapor-phase phosphorization method. The grown Ni2P NWAs with high sp. surface areas can not only offer ample active sites for the HER, but also serve as scaffolds for anchoring dye mols. to maximize the light utilization efficiency, which endows the Ni2P NWAs/NF monolithic cocatalyst with excellent HER activity. When sensitized with Erythrosin B (ErB) in triethanolamine (TEOA) solution, the turnover number (TON) of H2 evolution based on ErB reaches 9.7 in 5 h under visible light. Notably, the good structural integrity and inherent magnetism enable the Ni2P NWAs/NF to be easily separated from the reaction solution and excellent catalytic H2 evolution stability over a 45 h cycling reaction. This work presents a new strategy of fabricating monolithic cocatalysts with controllable microstructure and functionalities as well as high activity, durability, and device-compatibility for large-scale solar energy conversion applications. In the experiment, the researchers used many compounds, for example, Sodium 2′,4′,5′,7′-tetraiodo-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-bis(olate) (cas: 16423-68-0Recommanded Product: Sodium 2′,4′,5′,7′-tetraiodo-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-bis(olate)).

Sodium 2′,4′,5′,7′-tetraiodo-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-bis(olate) (cas: 16423-68-0) belongs to benzofurans derivatives. Benzofuran derivatives are one of the most important oxygen-containing heterocycles. In nature, benzofurans have occupied an important role among the plant phenols & several pharmacologically active compounds.Recommanded Product: Sodium 2′,4′,5′,7′-tetraiodo-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-3′,6′-bis(olate)

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

CC-1065 Analogues Bearing Different DNA-Binding Subunits: Synthesis, Antitumor Activity, and Preliminary Toxicity Study was written by Wang, Yuqiang;Li, Lianfa;Ye, Wenqing;Tian, Zhiming;Jiang, Wei;Wang, Hong;Wright, Susan C.;Larrick, James W.. And the article was included in Journal of Medicinal Chemistry in 2003.Name: 5-Fluorobenzofuran-2-carboxylic acid This article mentions the following:

CC-1065 analogs bearing different DNA-binding subunits were synthesized. A terminal C5-NO₂ and -F moiety at the DNA-binding subunit increased the drug’s potency and antitumor efficacy. A C5-OCH₃ reduced the potency and antitumor efficacy. Compound (±)-I, bearing a trans double bond, had increased antitumor efficacy. A preliminary toxicity study indicated that terminal C5-OCH₃ and -acetamido moieties at the DNA-binding subunit caused delayed death in mice. In the experiment, the researchers used many compounds, for example, 5-Fluorobenzofuran-2-carboxylic acid (cas: 89197-62-6Name: 5-Fluorobenzofuran-2-carboxylic acid).

5-Fluorobenzofuran-2-carboxylic acid (cas: 89197-62-6) 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. 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.Name: 5-Fluorobenzofuran-2-carboxylic acid

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Novel 2-arylbenzofuran dimers and polyisoprenylated flavanones from Sophora tonkinensis was written by Luo, Guoyong;Yang, Yun;Zhou, Min;Ye, Qi;Liu, Yan;Gu, Jian;Zhang, Guolin;Luo, Yinggang. And the article was included in Fitoterapia in 2014.Related Products of 6807-83-6 This article mentions the following:

Two novel 2-arylbenzofuran dimers, shandougenines A (1) and B (2), and two new polyisoprenylated flavanones 3 (shandougenine C) and 4 (shandougenine D) were isolated from the 95% EtOH extract of Sophora tonkinensis, together with 18 known compounds Their structures were determined on the basis of spectral data interpretation and by comparing the spectral data with that reported previously for known compounds Shandougenine A (1) is a unique dimeric 2-arylbenzofuran with a C-3-C-5”’ bond linkage. Shandougenine B (2) is the first naturally occurring dimeric 2-arylbenzofuran with a novel C-3-C-3” bond linkage. Compound 1 showed moderate DPPH free radical scavenging capacity, whereas 2 has stronger DPPH free radical and ABTS cation radical scavenging capacity than Vc. Compounds 12, 19, and 20 showed parallel DPPH free radical scavenging capacity with Vc. Compounds 1, 3, 4, 19, 20, and 22 have parallel ABTS cation radical scavenging capacity to Vc. Compounds 1, 3, 4, and 18 showed slightly stronger superoxide anion radical scavenging capacity than the known flavanone luteolin. The antioxidant activities of shandougenines A (1) and B (2) indicated that compounds 1 and 2 may represent novel scaffolds for the development of new antioxidants. In the experiment, the researchers used many compounds, for example, (2S,3R,4S,5S,6R)-2-(((6aR,12aR)-6a,12a-Dihydro-6H-[1,3]dioxolo[4′,5′:5,6]benzofuro[3,2-c]chromen-3-yl)oxy)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol (cas: 6807-83-6Related Products of 6807-83-6).

(2S,3R,4S,5S,6R)-2-(((6aR,12aR)-6a,12a-Dihydro-6H-[1,3]dioxolo[4′,5′:5,6]benzofuro[3,2-c]chromen-3-yl)oxy)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol (cas: 6807-83-6) 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.Related Products of 6807-83-6

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Small molecule probes to quantify the functional fraction of a specific protein in a cell with minimal folding equilibrium shifts was written by Liu, Yu;Tan, Yun Lei;Zhang, Xin;Bhabha, Gira;Ekiert, Damian C.;Genereux, Joseph C.;Cho, Younhee;Kipnis, Yakov;Bjelic, Sinisa;Baker, David;Kelly, Jeffery W.. And the article was included in Proceedings of the National Academy of Sciences of the United States of America in 2014.Application In Synthesis of 2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate This article mentions the following:

Although much is known about protein folding in buffers, it remains unclear how the cellular protein homeostasis network functions as a system to partition client proteins between folded and functional, soluble and misfolded, and aggregated conformations. Herein, we develop small mol. folding probes that specifically react with the folded and functional fraction of the protein of interest, enabling fluorescence-based quantification of this fraction in cell lysate at a time point of interest. Importantly, these probes minimally perturb a protein’s folding equilibrium within cells during and after cell lysis, because sufficient cellular chaperone/chaperonin holdase activity is created by rapid ATP depletion during cell lysis. The folding probe strategy and the faithful quantification of a particular protein’s functional fraction are exemplified with retroaldolase, a de novo designed enzyme, and transthyretin, a nonenzyme protein. Our findings challenge the often invoked assumption that the soluble fraction of a client protein is fully folded in the cell. Moreover, our results reveal that the partitioning of destabilized retroaldolase and transthyretin mutants between the aforementioned conformational states is strongly influenced by cytosolic proteostasis network perturbations. Overall, our results suggest that applying a chem. folding probe strategy to other client proteins offers opportunities to reveal how the proteostasis network functions as a system to regulate the folding and function of individual client proteins in vivo. In the experiment, the researchers used many compounds, for example, 2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate (cas: 92557-80-7Application In Synthesis of 2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate).

2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate (cas: 92557-80-7) belongs to benzofurans derivatives. Benzofuran is a core structural unit found in many naturally occurring compounds with multidirectional biological activities. Substituted benzofurans find applications such as fluorescent sensors, oxidants, in drug discovery, and in another field of chemistry and agriculture.Application In Synthesis of 2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Protein-responsive protein release of supramolecular/polymer hydrogel composite integrating enzyme activation systems was written by Shigemitsu, Hajime;Kubota, Ryou;Nakamura, Keisuke;Matsuzaki, Tomonobu;Minami, Saori;Aoyama, Takuma;Urayama, Kenji;Hamachi, Itaru. And the article was included in Nature Communications.Synthetic Route of C25H15NO9 This article mentions the following:

Non-enzymic proteins including antibodies function as biomarkers and are used as biopharmaceuticals in several diseases. Protein-responsive soft materials capable of the controlled release of drugs and proteins have potential for use in next-generation diagnosis and therapies. Here, we describe a supramol./agarose hydrogel composite that can release a protein in response to a non-enzymic protein. A non-enzymic protein-responsive system is developed by hybridization of an enzyme-sensitive supramol. hydrogel with a protein-triggered enzyme activation set. In situ imaging shows that the supramol./agarose hydrogel composite consists of orthogonal domains of supramol. fibers and agarose, which play distinct roles in protein entrapment and mech. stiffness, resp. Integrating the enzyme activation set with the composite allows for controlled release of the embedded RNase in response to an antibody. Such composite hydrogels would be promising as a matrix embedded in a body, which can autonomously release biopharmaceuticals by sensing biomarker proteins. In the experiment, the researchers used many compounds, for example, 2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate (cas: 92557-80-7Synthetic Route of C25H15NO9).

2,5-Dioxopyrrolidin-1-yl 3′,6′-dihydroxy-3-oxo-3H-spiro[isobenzofuran-1,9′-xanthene]-5-carboxylate (cas: 92557-80-7) 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 antioxidant, antitubercular, antiplasmodial, insecticidal.Synthetic Route of C25H15NO9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

A simple open source bioinformatic methodology for initial exploration of GPCR ligands′ agonistic/antagonistic properties was written by Panagiotopoulos, Athanasios A.;Papachristofi, Christina;Kalyvianaki, Konstantina;Malamos, Panagiotis;Theodoropoulos, Panayiotis A.;Notas, George;Calogeropoulou, Theodora;Castanas, Elias;Kampa, Marilena. And the article was included in Pharmacology Research & Perspectives in 2020.Quality Control of 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide This article mentions the following:

Drug development is an arduous procedure, necessitating testing the interaction of a large number of potential candidates with potential interacting (macro)mols. Therefore, any method which could provide an initial screening of potential candidate drugs might be of interest for the acceleration of the procedure, by highlighting interesting compounds, prior to in vitro and in vivo validation. In this line, we present a method which may identify potential hits, with agonistic and/or antagonistic properties on GPCR receptors, integrating the knowledge on signaling events triggered by receptor activation (GPCRs binding to Gα,β,γ proteins, and activating Gα, exchanging GDP for GTP, leading to a decreased affinity of the Gα for the GPCR). We show that, by integrating GPCR-ligand and Gα-GDP or -GTP binding in docking simulation, which correctly predicts crystallog. data, we can discriminate agonists, partial agonists, and antagonists, through a linear function, based on the ΔG (Gibbs-free energy) of liganded-GPCR/Gα-GDP. We built our model using two Gαs (β2-adrenergic and prostaglandin-D2), four Gαi (μ-opioid, dopamine-D3, adenosine-A1, rhodopsin), and one Gαo (serotonin) receptors and validated it with a series of ligands on a recently deorphanized Gαi receptor (OXER1). This approach could be a valuable tool for initial in silico validation and design of GPRC-interacting ligands. In the experiment, the researchers used many compounds, for example, 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide (cas: 179474-81-8Quality Control of 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide).

4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide (cas: 179474-81-8) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. 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.Quality Control of 4-Amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Development and characterization of layer-by-layer coated liposomes with poly(L-lysine) and poly(L-glutamic acid) to increase their resistance in biological media was written by Hermal, Florence;Frisch, Benoit;Specht, Alexandre;Bourel-Bonnet, Line;Heurtault, Beatrice. And the article was included in International Journal of Pharmaceutics (Amsterdam, Netherlands) in 2020.SDS of cas: 3326-34-9 This article mentions the following:

Multilayered coated liposomes were prepared using the layer-by-layer (LbL) technique in an effort to improve their stability in biol. media. The formulation strategy was based on the alternate deposition of two biocompatible and biodegradable polyelectrolytes – poly(L-lysine) (PLL) and poly(L-glutamic acid) (PGA) – on neg. charged small unilamellar vesicles (SUVs). Some parameters of the formulation process were optimized such as the polyelectrolyte concentration and the purification procedure. This optimized procedure has allowed the development of very homogeneous formulations of liposomes coated with up to 6 layers of polymers (so-called layersomes). The coating was characterized by dynamic light scattering (DLS), zeta potential measurements and Forster resonance energy transfer (FRET) between two fluorescently labeled polyelectrolytes. Studies on the stability of the formulations at 4°C in a buffered solution have shown that most structures are stable over 1 mo without impacting their encapsulation capacity. In addition, fluorophore release experiments have demonstrated a better resistance of the layersomes in the presence of a non-ionic detergent (Triton X-100) as well as in the presence of phospholipase A₂ and human plasma. In conclusion, new multilayered liposomes have been developed to increase the stability of conventional liposomes in biol. environments. In the experiment, the researchers used many compounds, for example, 5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 3326-34-9SDS of cas: 3326-34-9).

5-Amino-3′,6′-dihydroxy-3H-spiro[isobenzofuran-1,9′-xanthen]-3-one (cas: 3326-34-9) belongs to benzofurans derivatives. Many natural or synthetic compounds containing benzofuran skeletons have been found to possess remarkable activity as agrochemicals and pharmaceuticals. In nature, benzofurans have occupied an important role among the plant phenols & several pharmacologically active compounds.SDS of cas: 3326-34-9

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Nickel-catalyzed intramolecular C-H arylation using aryl pivalates as electrophiles was written by Wang, Jiayi;Ferguson, Devin M.;Kalyani, Dipannita. And the article was included in Tetrahedron in 2013.Safety of Naphtho[2,1-b]benzofuran This article mentions the following:

This paper describes a method for nickel catalyzed intramol. C-H arylation using aryl pivalates as electrophiles. The transformation is efficient for the synthesis of diverse electronically and sterically differentiated dibenzofurans. Addnl., the method could be expanded toward the synthesis of carbazoles. Preliminary mechanistic studies of the transformation are also described. In the experiment, the researchers used many compounds, for example, Naphtho[2,1-b]benzofuran (cas: 205-39-0Safety of Naphtho[2,1-b]benzofuran).

Naphtho[2,1-b]benzofuran (cas: 205-39-0) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Benzofurans are stable towards alkali and readily polymerize on treatment with sulfuric acid, due to which they are useful for the preparation of low cost chemically relatively inert resins.Safety of Naphtho[2,1-b]benzofuran

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem