34084-88-3

Usage

InChI:InChI=1/C10H7NO4S/c1-15-10(12)9-4-6-2-3-7(11(13)14)5-8(6)16-9/h2-5H,1H3

Upstream product

• 2365-48-2 Methyl thioglycolate 
• 157701-72-9 4-nitro-2-fluorobenzaldehyde 
• 67-56-1 methanol 
• 19983-42-7 6-nitrobenzo[b]thiophene-2-carboxylic acid 
• 528-75-6 2,4-dinitrobenzaldehyde 

Downstream Products

• 850073-52-8 6-[2-(4-phenyl-piperazin-1-yl)-acetylamino]-benzo[b]thiophene-2-carboxylic acid hydroxyamide 
• 850073-48-2 6-dibenzylamino-benzo[b]thiophene-2-carboxylic acid hydroxyamide 
• 850073-47-1 6-dibenzylamino-benzo[b]thiophene-2-carboxylic acid methyl ester 
• 913653-80-2 N-hydroxy-6-{[{[(4-methylphenyl)sulfonyl]amino}(phenyl)acetyl]amino}-1-benzothiophene-2-carboxamide 
• 913653-79-9 tert-butyl [(1S)-1-benzyl-2-({2-[(hydroxyamino)carbonyl]-1-benzothien-6-yl}amino)ethyl]carbamate 
• 19983-42-7 6-nitrobenzo[b]thiophene-2-carboxylic acid 
• 1436433-47-4 C₁₇H₉Cl₂N₃O₂S₂ 
• 1436433-46-3 C₁₇H₉Cl₂N₃O₂S₂ 
• 1436433-45-2 C₁₇H₉BrClN₃O₂S₂ 
• 1436433-44-1 C₁₇H₁₀FN₃O₂S₂ 
• 1436433-43-0 C₁₇H₁₀ClN₃O₂S₂ 
• 1436433-42-9 C₁₇H₁₀BrN₃O₂S₂ 
• 1436433-41-8 C₁₇H₁₀BrN₃O₂S₂ 
• 1436433-40-7 C₂₃H₁₅N₃O₃S₂ 

Relevant academic research and scientific papers

Discovery of fluorescent coumarin-benzo[b]thiophene 1, 1-dioxide conjugates as mitochondria-targeting antitumor STAT3 inhibitors

STAT3 has been extensively studied as a potential antitumor target. Though studies on regulating STAT3 mainly focus on the inhibition of STAT3 phosphorylation at Tyr705 residue, the phosphorylation at Ser727 residue of STAT3 protein is also closely associated with the mitochondrial import of STAT3 protein. N, N-diethyl-7-aminocoumarin is a fluorescent mitochondria-targeting probe. In this study, a series of STAT3 inhibitors were developed by connecting N, N-diethyl-7-aminocoumarin fluorophore with benzo [b]thiophene 1, 1-dioxide moiety. All designed compounds displayed potent anti-proliferative activity against cancer cells. The representative compound 7a was mainly accumulated in mitochondria visualized by its fluorescence. STAT3 phosphorylation was inhibited by compound 7a at both Tyr705 and Ser727 residues. Compound 7a inhibited STAT3 phosphorylation whereas had no influence on the phosphorylation levels of STAT1, JAK2, Src and Erk1/2, indicating good selectivity of compound 7a. Moreover, compound 7a down-regulated the expression of STAT3 target genes Bcl-2 and Cyclin D1, increased ROS production and remarkably reduced the mitochondrial membrane potential to induce mitochondrial apoptotic pathway. Furthermore, compound 7a in vivo suppressed breast cancer 4T1 implanted tumor growth. Taken together, these results highlighted that compound 7a might be a promising mitochondria-targeting STAT3 inhibitor for cancer therapy.

GEMINAL SUBSTITUTED QUINUCLIDINE AMIDE COMPOUNDS AS AGONISTS OF ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTORS

The present invention relates to novel geminal substituted quinuclidine amide compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of α7- nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.

HETEROCYCLIC DERIVATIVES AND USE THEREOF

A heterocyclic derivative represented by formula (I), or a pharmaceutically acceptable salt or a stereoisomer thereof, which has an inhibitory effect on the activation of STAT3 protein, and is useful for the prevention or treatment of diseases associated with the activation of STAT3 protein.

Discovery of protein-protein interaction inhibitors of replication protein A

Replication protein A (RPA) is a ssDNA binding protein that is essential for DNA replication and repair. The initiation of the DNA damage response by RPA is mediated by protein-protein interactions involving the N-terminal domain of the 70 kDa subunit with partner proteins. Inhibition of these interactions increases sensitivity toward DNA damage and replication stress and may therefore be a potential strategy for cancer drug discovery. Toward this end, we have discovered two lead series of compounds, derived from hits obtained from a fragment-based screen, that bind to RPA70N with low micromolar affinity and inhibit the binding of an ATRIP-derived peptide to RPA. These compounds may offer a promising starting point for the discovery of clinically useful RPA inhibitors.

Discovery of a new series of potent and selective linear tachykinin NK 2 receptor antagonists

Starting from 1 (MEN 14268), a selective tachykinin NK2 receptor antagonist with an interesting in vitro pharmacological profile, a family of numerous antagonists was obtained through an optimization process focused on iterated structural modifications. The effects of the introduction of a wide variety of substituents on the lipophilic aromatic part of the molecule and the modulation of the structural constraint through the insertion of different achiral α,α-dialkylamino acids were investigated. In particular, aromatic and benzofused heteroaromatic moieties were introduced at the pseudo-N-terminal residue to replace the 2-benzothiophene moiety, and a systematic investigation of the best positioning of substituents onto the aromatic platform was reported for the benzothiophene core. Studies on the modulation of the length and the rigidity of the hydrophilic pseudo-C-terminal pendant are presented. Many heteroaliphatic groups are well tolerated by the receptor in this part of the ligand. The product 48f (MEN15596), bearing a methyl substituent on the benzothiophene and a tetrahydropyranylmethylpiperidine pendant, was finally selected for its good in vivo activity after intravenous, intraduodenal, and oral administration in guinea pigs.

BENZOTHIOPHENE HYDROXAMIC ACID DERIVATIVES

The present invention relates to a novel class of hydroxamic acid derivatives. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing t

BENZOTHIOPHENE HYDROXAMIC ACID DERIVATIVES WITH CARBAMATE, UREA, AMIDE AND SULFONAMIDE SUBSTITUTIONS

The present invention relates to a novel class of hydroxamic acid derivatives carbamate, urea, amide and sulfonamide substitutions. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetyla

BENZOTHIOPHENE DERIVATIVES

The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.

THIOPHENE AND BENZOTHIOPHENE HYDROXAMIC ACID DERIVATIVES

The present invention relates to a novel class of hydroxamic acid derivatives having a benzothiophene or thiophene backbone. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit historic deacetylase and

BENZOTHIOPHENE UREA, BENZOFURANE UREA, AND INDOLE UREA, AND USE OF THE SAME AS ALPHA-7 ACHR AGONISTS

The invention relates to novel benzothiophene urea, benzofurane urea, and indole urea, and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration power, learning capacity and/or memory retention.