171349-95-4Relevant academic research and scientific papers
Metal-Free Direct Trifluoromethylthiolation of Aromatic Compounds Using Triptycenyl Sulfide Catalyst
Kurose, Ryo,Nishii, Yuji,Miura, Masahiro
supporting information, p. 2380 - 2385 (2021/04/05)
Herein we report an efficient synthetic method for the electrophilic trifluoromethylthiolation of aromatic compounds. The key is to use triptycenyl sulfide (Trip-SMe) and TfOH to enhance the electrophilicity of SCF3 fragment through the formation of sulfonium intermediates. This method enables direct installation of an SCF3 group onto unactivated aromatics at room temperature, adopting a commercially available saccharin-based reagent. Preliminary DFT calculation was carried out to investigate the substitution effect on the catalytic activity.
Structural development of N-(4-phenoxyphenyl)benzamide derivatives as novel SPAK inhibitors blocking WNK kinase signaling
Fujii, Shinya,Ishigami-Yuasa, Mari,Isobe, Kiyoshi,Kagechika, Hiroyuki,Kikuchi, Eriko,Mori, Takayasu,Suzuyama, Honoka,Uchida, Shinichi,Watanabe, Yuko
supporting information, (2020/07/21)
We report here structural development of N-(4-phenoxyphenyl)benzamide derivatives as novel SPAK (STE20/SPS1-related proline/alanine-rich kinase) inhibitors. Abnormal activation of the signal cascade of with-no-lysine kinase (WNK) with OSR1 (oxidative stress-responsive kinase 1)/SPAK and NCC (NaCl cotransporter) results in characteristic salt-sensitive hypertension, and therefore inhibitors of the WNK-OSR1/SPAK-NCC cascade are candidates for antihypertensive drugs. Based on the structure of lead compound 2, we examined the SAR of N-(4-phenoxyphenyl)benzamide derivatives, and developed compound 20l as a potent SPAK inhibitor. Compounds 20l is a promising candidate for a new class of antihypertensive drugs.
QUINAZOLINE DERIVATIVES AS TYROSINE KINASE INHIBITOR, COMPOSITIONS, METHODS OF MAKING THEM AND THEIR USE
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Page/Page column 521-522, (2020/05/13)
The present disclosure relates to new compounds or pharmaceutically acceptable salts or stereoisomers thereof of formula I as inhibitors of receptor tyrosine kinases (RTK), in particular extracellular mutants of ErbB-receptors. The present disclosure also relates to methods of preparation these compounds, compositions comprising these compounds, and methods of using them in the treatment of cancer in mammals (e.g. humans).
Targeting Myeloid Differentiation Using Potent 2-Hydroxypyrazolo[1,5- a]pyridine Scaffold-Based Human Dihydroorotate Dehydrogenase Inhibitors
Sainas, Stefano,Pippione, Agnese C.,Lupino, Elisa,Giorgis, Marta,Circosta, Paola,Gaidano, Valentina,Goyal, Parveen,Bonanni, Davide,Rolando, Barbara,Cignetti, Alessandro,Ducime, Alex,Andersson, Mikael,J?rv?, Michael,Friemann, Rosmarie,Piccinini, Marco,Ramondetti, Cristina,Buccinnà, Barbara,Al-Karadaghi, Salam,Boschi, Donatella,Saglio, Giuseppe,Lolli, Marco L.
supporting information, p. 6034 - 6055 (2018/07/05)
Human dihydroorotate dehydrogenase (hDHODH) catalyzes the rate-limiting step in de novo pyrimidine biosynthesis, the conversion of dihydroorotate to orotate. hDHODH has recently been found to be associated with acute myelogenous leukemia, a disease for wh
CAPREOMYCIN DERIVATIVES AND THEIR USE AS ANTIBACTERIALS
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Page/Page column 92, (2008/06/13)
The present invention relates to phenylurea derivatives of capreomycin I, IIB, IIA, or IB, and metabolites and pharmaceutically acceptable salts and solvates thereof. The compounds of the present invention are useful as antibacterial agents for treating b
Capreomycin derivatives and their use as antibacterials
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Page/Page column 47, (2008/06/13)
The present subject matter relates to phenylurea capreomycin derivatives, and to metabolites and pharmaceutically acceptable salts and solvates thereof. The compounds of the present subject matter are useful as antibacterial agents for treating bacterial
Substituted bicyclic derivatives useful as anticancer agents
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, (2008/06/13)
The invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X, R1, R3and R4are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals with administering the compounds of formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1.
