New explortion of 3-Methylbenzofuran-2-carbaldehyde

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COMPOUNDS, COMPOSITIONS, AND METHODS FOR MODULATING CFTR

The present disclosure is directed to disclosed compounds that modulate, e.g., address underlying defects in cellular processing of CFTR activity.

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Reference£º
Benzofuran – Wikipedia,
Benzofuran | C8H1563O – PubChem

Simple exploration of 3-Methylbenzofuran-2-carbaldehyde

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Cycloisomerization between Aryl Enol Ether and Silylalkynes under Ruthenium Hydride Catalysis: Synthesis of 2,3-Disubstituted Benzofurans

Metal-catalyzed cycloisomerization reactions of 1,n-enynes have become conceptually and chemically attractive processes in the search for atom economy, which is a key subject of current research. However, metal-catalyzed cycloisomerization between aryl enol ether and silylalkynes has not been developed. The ruthenium hydride complex catalyzed cycloisomerization between aryl enol ether and silylalkynes is reported to give benzofurans having useful functional groups, vinyl and trimethylsilylmethyl, on the 2- and 3-positions, respectively.

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Benzofuran – Wikipedia,
Benzofuran | C8H1573O – PubChem

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HETEROCYCLIC COMPOUNDS AS INHIBITORS OF FATTY ACID BIOSYNTHESIS FOR BACTERIAL INFECTIONS

The present invention relates to novel heterocyclic compounds which specifically inhibit bacterial Fab I and can be used for the treatment of Staphylococcal infections.

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Benzofuran – Wikipedia,
Benzofuran | C8H1565O – PubChem

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Access to Hetero-Benzyl Scaffolds via Transient-Ligand-Enabled Direct gamma-C(sp3)-H Arylation of 3-Methylheteroarene-2-Carbaldehydes

An efficient and straightforward method has been developed for the synthesis of beta-benzyl-substituted 5-membered heterocyclic carbaldehydes via transient directing-group-enabled direct gamma-C(sp3)-H arylation of 3-methylheteroarene-2-carbaldehydes. A wide range of 3-methylheteroarene carbaldehydes undergo coupling with a variety of aryl iodides, including less reactive iodo pyridine derivatives to provide a library of highly selective functionalized products in good to excellent yields. Some of these products have been successfully utilized in synthesizing useful synthetic intermediates.

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Benzofuran – Wikipedia,
Benzofuran | C8H1574O – PubChem

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HETEROCYCLIC COMPOUNDS AS INHIBITORS OF FATTY ACID BIOSYSNTHESIS FOR BACTERIAL INFECTIONS

The present invention relates to novel heterocyclic compounds which specifically inhibit bacterial FabI and can be used for the treatment of Staphylococcal infections.

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Benzofuran – Wikipedia,
Benzofuran | C8H1566O – PubChem

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Therapeutic reactivation of mutant p53 protein by quinazoline derivatives

Summary: Purpose The human tumour suppressor protein p53 is mutated in nearly half of human tumours and most mutant proteins have single amino acid changes. Several drugs including the quinazoline derivative 1 (CP-31398) have been reported to restore p53 activity in mutant cells. The side chain of 1 contains a styryl linkage that compromises its stability and we wished to explore the activity of analogues containing more stable side chains. Methods Reactivation of p53 function was measured by flow cytometry as the ability to potentiate radiation-induced G1-phase cell cycle arrest and by western blotting to determine expression of p21WAF1. DNA binding was measured by competition with ethidium and preliminary pharmacological and xenograft studies were carried out. Results Screening of analogues for potentiation of radiation-induced G1-phase cell cycle arrest using NZOV11, an ovarian tumour cell line containing a p53R248Q mutation, demonstrated that the (2-benzofuranyl)-quinazoline derivative 5 was among the most active of the analogues. Compound 5 showed similar effects in several other p53 mutant human tumour cell lines but not in a p53 null cell line. 5 also potentiated p21WAF1 expression induced by radiation. DNA binding affinity was measured and found to correlate with p53 reactivation activity. Plasma concentrations of 5 in mice were sufficient to suggest in vivo activity and a small induced tumour growth delay (7 days) of NZM4 melanoma xenografts was observed. Conclusion Compound 5 restores p53-like function to a human tumour cells lines expressing a variety of mutant p53 proteins, thus providing a basis for the design of further new drugs.

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Benzofuran – Wikipedia,
Benzofuran | C8H1579O – PubChem