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TTK kinase was identified by in-house siRNA screen and pursued as a tractable, novel target for cancer treatment. A screening campaign and systematic optimization, supported by computer modeling led to an indazole core with key sulfamoylphenyl and acetamido moieties at positions 3 and 5, respectively, establishing a novel chemical class culminating in identification of 72 (CFI-400936). This potent inhibitor of TTK (IC50 = 3.6 nM) demonstrated good activity in cell based assay and selectivity against a panel of human kinases. A co-complex TTK X-ray crystal structure and results of a xenograft study with TTK inhibitors from this class are described.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Novel thiophene and benzothiophene containing diphosphine ligands 5-8 with a chiral cyclohexyl diamine backbone have been prepared and used in the asymmetric allylation of catechol. The advantage of these new ligands is their high reactivity and excellent selectivity. The best results were obtained using ligand 7 to give the allylated catechol 24b from 23b in 90% ee and 91% yield within 4 hours.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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A method for the Pd-catalyzed arylation of ammonia with a wide range of aryl and heteroaryl halides, including challenging five-membered heterocyclic substrates, is described. Excellent selectivity for monoarylation of ammonia to primary arylamines was achieved under mild conditions or at rt by the use of bulky biarylphosphine ligands (L6, L7, and L4) as well as their corresponding aminobiphenyl palladacycle precatalysts (3a, 3b, and 3c). As this process requires neither the use of a glovebox nor high pressures of ammonia, it should be widely applicable.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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STAT3 is an attractive therapeutic target for cancer therapy. However, due to low potency or poor druggability, none of its inhibitors are clinically available. Herein, a series of aminobenzo[b]thiophene 1, 1-dioxides with good drug-likeness properties were designed, synthesized and evaluated as STAT3 inhibitors. Most of them exhibited higher antitumor activity than the small-molecule STAT3 inhibitor, Stattic. Compound 15 was the most potent and had an IC50range in 0.33?0.75 muM in various cancer cell lines. The overexpressed and IL-6 induced phosphorylation levels of STAT3 were both inhibited by 15 without influencing the phosphorylation levels of the upstream kinases Src and Jak2. 15 also suppressed the expressions of STAT3 downstream gene, Bcl-2. 15 effectively increased the ROS levels of cancer cells, induced cancer cell apoptosis and abolished the colony formation ability of cancer cells without affecting bypass kinase p-Erk. Furthermore, 15 in vivo induced significant antitumor responses, and exhibited less toxicity than Doxorubicin. Together, this study described a class of new STAT3 inhibitors as antitumor agents.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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GPR40 partial agonism is a promising new mechanism for the treatment of type 2 diabetes mellitus with clinical proof of concept. Most of the GPR40 agonists in the literature have a carboxylic acid functional group, which may pose a risk for idiosyncratic drug toxicity. A novel series of GPR40 agonists containing a tetrazole as a carboxylic acid bioisostere was identified. This series of compounds features a benzo[b]thiophene as the center ring, which is prone to oxidation during phase 1 metabolism. Following SAR optimization targeting GPR40 agonist activity and intrinsic clearance in microsomes (human and rat), potent and metabolically stable compounds were selected for in vivo evaluation. The compounds are efficacious at lowering blood glucose in a SD rat oGTT model.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Compositions including derivatives of spinosyns of the following formulae and methods for the production of derivatives of spinosyns are provided. The spinosyn derivatives described herein include those functionalized on the C-5,6 double bond to provide an aziridine ring system. The method produces spinosyn derivatives that exhibit activity towards insects, arachnids, and nematodes and are useful in the agricultural and animal health markets.

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Benzothiophene – Wikipedia,
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PURPOSE: A compound for an organic optoelectronic device is provided to efficiently inject or transfer electrons, and to offer high electrochemical stability, lifetime, and efficiency. CONSTITUTION: A compound is denoted by chemical formula 1. In the chemical formula 1: X^2 is N, B, or P; X^1 is O, S, S (O), S (O2), or NR’; R^1-R^9 are hydrogen, deuterium, a substituted or non-substituted C1-10 alkyl group, a substituted or non-substituted C6-30 aryl group, or a substituted or non-substituted C2-30 heteroaryl group; L^1 is a substituted or non-substituted C6-30 arylene group, or a substituted or non-substituted C2-30 heteroarylene group; and L^2 and L^3 are a single bond, a substituted or non-substituted C2-10 alkenylene group, a substituted or non-substituted C2-10 alkynylene group, a substituted or non-substituted C6-30 arylene group, or a substituted or non-substituted C2-30 heteroarylene group.

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Benzothiophene – Wikipedia,
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The reaction of aryllithium reagents prepared by halogen metal exchange or direct metallation with alpha,alpha,alpha-trifluoro-N,N-dimethylacetamide give the corresponding aryltrifluoromethylketones in good yield.

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Benzothiophene – Wikipedia,
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The invention relates to an optical functional material field, in particular to a infrared BODIPY dye, having the formula (1) the structure of the shown, wherein R1 And R2 C independent of each other1 – C10 Alkyl, aromatic or heteroaromatic group in the a; R3 For the H atom, C1 – C10 Hydrocarbyl or aromatic-based one. The fluorescent dye of the ultraviolet visible absorption spectrum and fluorescence emission spectrum is narrow, molar absorption coefficient is high, the fluorescence quantum efficiency is high, and the light stability is good, trace detection, high sensitivity, can be used for cell imaging, fluorescent probe, laser dye, fluorescent sensor and the near infrared light dynamics and so different application areas, demonstrate good practicability. (by machine translation)

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula -X3-X4- or -X4-X3-, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP-13 production inhibitory effect.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem