Application of 847818-74-0In 2015 ,《Discovery of novel quinoline-based mTOR inhibitors via introducing intra-molecular hydrogen bonding scaffold (iMHBS): The design, synthesis and biological evaluation》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Ma, Xiaodong; Lv, Xiaoqing; Qiu, Ni; Yang, Bo; He, Qiaojun; Hu, Yongzhou. The article conveys some information:
A series of quinoline derivatives featuring the novelty of introducing intra-mol. hydrogen bonding scaffold (iMHBS) were designed, synthesized and biol. evaluated for their mTOR inhibitory activity, as well as anti-proliferative efficacies against HCT-116, PC-3 and MCF-7 cell lines. As a result, six compounds exhibited significant inhibition against mTOR with IC50 values below 35 nM. Hydrochloride of 4′-((4-(piperazin-1-yl)-3-(trifluoromethyl)phenyl)amino)-[3,6′-biquinoline]-3′-carboxamide (compound 15a), the most potent mTOR inhibitor reported herein (IC50 = 14 nM), also displayed the most favorable cellular activities, with the IC50 values of 0.46, 0.61 and 0.24 μM against HCT-116, PC-3 and MCF-7, resp. Besides, several compounds in this series were identified to be selective over class I PI3Ks. Further western blot anal. of 4′-((4-(4-acetylpiperazin-1-yl)-3-(trifluoromethyl)phe- nyl)amino)-[3,6′-biquinoline]-3′-carboxamide (compound 16b), a representative compound in this series, highlighted their advantage in surmounting the S6K/IRS1/PI3K neg. feedback loop upon dual inhibition of mTORC1 and mTORC2. In addition to the remarkable activity, (compound 15a) demonstrated acceptable stability in simulated gastric fluid (SGF), simulated intestinal fluid (SIF) and liver microsome, thereby being valuable for extensive in vivo investigation. In the experimental materials used by the author, we found 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Application of 847818-74-0)
1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, antipyretic, neuroleptic, anticonvulsant, antiarrhythmic, sedative, muscle relaxant, monoamine oxidase inhibitory, anti-inflammatory, antidiabetic and antibacterial activities. Application of 847818-74-0
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics