Tag: M.W=250-300

Pan, Bo-Sheng’s team published research in Science (Washington, DC, United States) in 369 | CAS: 129425-81-6

Science (Washington, DC, United States) published new progress about 129425-81-6. 129425-81-6 belongs to benzothiophene, auxiliary class Inhibitor, name is 4-(5,6-Dimethoxybenzo[b]thiophen-2-yl)-4-oxobutanoic acid, and the molecular formula is C14H14O5S, Synthetic Route of 129425-81-6.

Pan, Bo-Sheng published the artcileAn orally available non-nucleotide STING agonist with antitumor activity, Synthetic Route of 129425-81-6, the publication is Science (Washington, DC, United States) (2020), 369(6506), eaba6098, database is CAplus and MEDLINE.

Pharmacol. activation of the STING (stimulator of interferon genes)-controlled innate immune pathway is a promising therapeutic strategy for cancer. Here we report the identification of MSA-2, an orally available non-nucleotide human STING agonist. In syngeneic mouse tumor models, s.c. and oral MSA-2 regimens were well tolerated and stimulated interferon-β secretion in tumors, induced tumor regression with durable antitumor immunity, and synergized with anti-PD-1 therapy. Exptl. and theor. analyses showed that MSA-2 exists as interconverting monomers and dimers in solution, but only dimers bind and activate STING. This model was validated by using synthetic covalent MSA-2 dimers, which were potent agonists. Cellular potency of MSA-2 increased upon extracellular acidification, which mimics the tumor microenvironment. These properties appear to underpin the favorable activity and tolerability profiles of effective systemic administration of MSA-2.

Science (Washington, DC, United States) published new progress about 129425-81-6. 129425-81-6 belongs to benzothiophene, auxiliary class Inhibitor, name is 4-(5,6-Dimethoxybenzo[b]thiophen-2-yl)-4-oxobutanoic acid, and the molecular formula is C14H14O5S, Synthetic Route of 129425-81-6.

Referemce:
https://en.wikipedia.org/wiki/Benzothiophene,
Benzothiophene | C8H6S – PubChem

 

Cherney, Emily C.’s team published research in Journal of Medicinal Chemistry in 65 | CAS: 129425-81-6

Journal of Medicinal Chemistry published new progress about 129425-81-6. 129425-81-6 belongs to benzothiophene, auxiliary class Inhibitor, name is 4-(5,6-Dimethoxybenzo[b]thiophen-2-yl)-4-oxobutanoic acid, and the molecular formula is C14H14O5S, Category: benzothiophene.

Cherney, Emily C. published the artcileDiscovery of Non-Nucleotide Small-Molecule STING Agonists via Chemotype Hybridization, Category: benzothiophene, the publication is Journal of Medicinal Chemistry (2022), 65(4), 3518-3538, database is CAplus and MEDLINE.

The identification of agonists of the stimulator of interferon genes (STING) pathway has been an area of intense research due to their potential to enhance innate immune response and tumor immunogenicity in the context of immuno-oncol. therapy. Initial efforts to identify STING agonists focused on the modification of 2′,3′-cGAMP (1) (an endogenous STING activator ligand) and other closely related cyclic dinucleotides (CDNs). While these efforts have successfully identified novel CDNs that have progressed into the clinic, their utility is currently limited to patients with solid tumors that STING agonists can be delivered to intratumorally. Herein, we report the discovery of a unique class of non-nucleotide small-mol. STING agonists that demonstrate antitumor activity when dosed intratumorally in a syngeneic mouse model.

Journal of Medicinal Chemistry published new progress about 129425-81-6. 129425-81-6 belongs to benzothiophene, auxiliary class Inhibitor, name is 4-(5,6-Dimethoxybenzo[b]thiophen-2-yl)-4-oxobutanoic acid, and the molecular formula is C14H14O5S, Category: benzothiophene.

Referemce:
https://en.wikipedia.org/wiki/Benzothiophene,
Benzothiophene | C8H6S – PubChem

 

Syeda, Madiha Zahra’s team published research in Nano Research in | CAS: 129425-81-6

Nano Research published new progress about 129425-81-6. 129425-81-6 belongs to benzothiophene, auxiliary class Inhibitor, name is 4-(5,6-Dimethoxybenzo[b]thiophen-2-yl)-4-oxobutanoic acid, and the molecular formula is C5H7NO, Name: 4-(5,6-Dimethoxybenzo[b]thiophen-2-yl)-4-oxobutanoic acid.

Syeda, Madiha Zahra published the artcileA prodrug nanoplatform via esterification of STING agonist and IDO inhibitor for synergistic cancer immunotherapy, Name: 4-(5,6-Dimethoxybenzo[b]thiophen-2-yl)-4-oxobutanoic acid, the publication is Nano Research, database is CAplus.

Cancer immunotherapy has made significant progress in the last few decades, revolutionizing oncol. However, low patient response rates and potential immune-related adverse events continue to be major clin. challenges. Cancer nanomedicine, by virtue of its regulated delivery and modular flexibility, has shown the potential to strengthen antitumor immune responses and sensitize tumors to immunotherapy. In this study, we developed tumor microenvironment (TME) responsive nanomedicine to achieve specific and localized amplification of the immune response in tumor tissue in a safe and effective manner, while simultaneously reducing immune-related side effects. We synthesized the TME responsive prodrug by coupling MSA-2, a stimulator of interferon genes (STING) agonist, and NLG-919, an indoleamine 2,3 dioxygenase (IDO) inhibitor. The prodrug was assembled into nanoparticles to enhance the solubility and bioavailability. By synthesizing a TME responsive prodrug, we aim to explore the therapeutic efficacy of combined regimen (STING agonist and IDO inhibitor) for cancer, and reduce the unwanted side effects of STING agonism on normal tissues. Free prodrug and nanoparticles were characterized by mass spectrometry, dynamic light scattering (DLS), and transmission electron microscopy (TEM). Following that, we investigated the tumor accumulation, anti-tumor activity, and toxicity in vitro and in vivo. Prodrug nanoparticles demonstrated the ability to inhibit the tumor growth and activate antitumor immune response by modulating immune cells populations in tumor microenvironment. The TME responsive nanomedicine provided an effective tool for precise targeting, promoting antitumor immunity, and efficient tumor growth inhibition with safety. Outcomes of this study may have implications for future clin. trials.

Nano Research published new progress about 129425-81-6. 129425-81-6 belongs to benzothiophene, auxiliary class Inhibitor, name is 4-(5,6-Dimethoxybenzo[b]thiophen-2-yl)-4-oxobutanoic acid, and the molecular formula is C5H7NO, Name: 4-(5,6-Dimethoxybenzo[b]thiophen-2-yl)-4-oxobutanoic acid.

Referemce:
https://en.wikipedia.org/wiki/Benzothiophene,
Benzothiophene | C8H6S – PubChem

 

Meyer, Michael D.’s team published research in Journal of Medicinal Chemistry in 2000-04-20 | CAS: 67189-92-8

Journal of Medicinal Chemistry published new progress about Pharmacophores. 67189-92-8 belongs to class benzothiophene, name is Ethyl 3-amino-4-chlorobenzo[b]thiophene-2-carboxylate, and the molecular formula is C11H10ClNO2S, Computed Properties of 67189-92-8.

Meyer, Michael D. published the artcileStructure-Activity Studies for a Novel Series of Tricyclic Substituted Hexahydrobenz[e]isoindole α1A Adrenoceptor Antagonists as Potential Agents for the Symptomatic Treatment of Benign Prostatic Hyperplasia (BPH), Computed Properties of 67189-92-8, the main research area is alpha1A adrenoceptor uroselective hexahydrobenzisoindole synthesis.

In search of a uroselective agent that exhibits a high level of selectivity for the α1A receptor, a novel series of tricyclic hexahydrobenz[e]isoindoles was synthesized. A generic pharmacophoric model was developed requiring the presence of a basic amine core and a fused heterocyclic side chain separated by an alkyl chain. It was shown that the 6-OMe substitution with R, R stereochem. of the ring junction of the benz[e]isoindole and a two-carbon spacer chain were optimal. In contrast to the highly specific requirements for the benz[e]isoindole portion and linker chain, a wide variety of tricyclic fused heterocyclic attachments were tolerated with retention of potency and selectivity. In vitro functional assays for the α1 adrenoceptor subtypes were used to further characterize these compounds, and in vivo models of vascular vs prostatic tone were used to assess uroselectivity.

Journal of Medicinal Chemistry published new progress about Pharmacophores. 67189-92-8 belongs to class benzothiophene, name is Ethyl 3-amino-4-chlorobenzo[b]thiophene-2-carboxylate, and the molecular formula is C11H10ClNO2S, Computed Properties of 67189-92-8.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Nishida, K.’s team published research in Journal of the Society of Dyers and Colourists in 1978-06-30 | CAS: 67189-92-8

Journal of the Society of Dyers and Colourists published new progress about Acetate fibers Role: USES (Uses). 67189-92-8 belongs to class benzothiophene, name is Ethyl 3-amino-4-chlorobenzo[b]thiophene-2-carboxylate, and the molecular formula is C11H10ClNO2S, Synthetic Route of 67189-92-8.

Nishida, K. published the artcileDyeing properties of disperse dyes derived from substituted 3-aminobenzo[b]thiophenes, Synthetic Route of 67189-92-8, the main research area is benzothiophene azo disperse dye; acetate fiber dye; polyamide fiber dye.

Six disperse azo dyes (I; R = CN, Ac, CO2Et, CO2H; R1 = H, Cl) λ 400-517 nm (EtOH) were prepared by coupling m-MeC6H4N(CH2CH2OH)CH2CH2CN [119-95-9] with diazotized 3-aminobenzo[b]thiophenes and their dyeing properties on acetate and nylon 6 fibers determined Most of the dyes showed good substantivity for both fibers, exhausting well to give bright dyeings of good general fastness; some showed higher lightfastness and brighter colors on acetate than on nylon 6.

Journal of the Society of Dyers and Colourists published new progress about Acetate fibers Role: USES (Uses). 67189-92-8 belongs to class benzothiophene, name is Ethyl 3-amino-4-chlorobenzo[b]thiophene-2-carboxylate, and the molecular formula is C11H10ClNO2S, Synthetic Route of 67189-92-8.

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem