Category: 844501-71-9

Reference of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleIn 2009 ,《A convenient and rapid approach for the synthesis of 1-benzyl-3-heterocyclic pyrazoles》 appeared in Tetrahedron Letters. The author of the article were Curtis, Michael P.; Sammons, Matthew F.; Piotrowski, David W.. The article conveys some information:

A variety of 1-benzyl-3-hetarylpyrazoles were rapidly assembled by a 2-step N-benzylation/Suzuki coupling sequence using a 3-pyrazolylboronate and benzyl bromides as starting compounds A 1-pot variation of this sequence is demonstrated. The results came from multiple reactions, including the reaction of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Reference of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole)

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) 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. Reference of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Reference of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleIn 2009 ,《A convenient and rapid approach for the synthesis of 1-benzyl-3-heterocyclic pyrazoles》 appeared in Tetrahedron Letters. The author of the article were Curtis, Michael P.; Sammons, Matthew F.; Piotrowski, David W.. The article conveys some information:

A variety of 1-benzyl-3-hetarylpyrazoles were rapidly assembled by a 2-step N-benzylation/Suzuki coupling sequence using a 3-pyrazolylboronate and benzyl bromides as starting compounds A 1-pot variation of this sequence is demonstrated. The results came from multiple reactions, including the reaction of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Reference of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole)

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) 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. Reference of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Application of 844501-71-9In 2016 ,《Overcoming resistance to HER2 inhibitors through state-specific kinase binding》 appeared in Nature Chemical Biology. The author of the article were Novotny, Chris J.; Pollari, Sirkku; Park, Jin H.; Lemmon, Mark A.; Shen, Weijun; Shokat, Kevan M.. The article conveys some information:

The heterodimeric receptor tyrosine kinase complex formed by HER2 and HER3 can act as an oncogenic driver and is also responsible for rescuing a large number of cancers from a diverse set of targeted therapies. Inhibitors of these proteins, particularly HER2, have dramatically improved patient outcomes in the clinic, but recent studies have demonstrated that stimulating the heterodimeric complex, either via growth factors or by increasing the concentrations of HER2 and HER3 at the membrane, significantly diminishes the activity of the inhibitors. To identify an inhibitor of the active HER2-HER3 oncogenic complex, the authors developed a panel of Ba/F3 cell lines suitable for ultra-high-throughput screening. Medicinal chem. on the hit scaffold resulted in a previously uncharacterized inhibitor that acts through preferential inhibition of the active state of HER2 and, as a result, is able to overcome cellular mechanisms of resistance such as growth factors or mutations that stabilize the active form of HER2. In the experiment, the researchers used 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Application of 844501-71-9)

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Application of 844501-71-9

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Che, Jinxin; Dai, Xiaoyang; Gao, Jian; Sheng, Haichao; Zhan, Wenhu; Lu, Yang; Li, Dan; Gao, Zizheng; Jin, Zegao; Chen, Binhui; Luo, Peihua; Yang, Bo; Hu, Yongzhou; He, Qiaojun; Weng, Qinjie; Dong, Xiaowu published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Discovery of N-((3S,4S)-4-(3,4-Difluorophenyl)piperidin-3-yl)-2-fluoro-4-(1-methyl-1H-pyrazol-5-yl)benzamide (Hu7691), a Potent and Selective Akt Inhibitor That Enables Decrease of Cutaneous Toxicity》.Electric Literature of C9H15BN2O2 The article contains the following contents:

Here, the inhibition of Akt2 isoenzyme might be a driver for keratinocyte apoptosis was demonstrate, which promotes us to search for new selective Akt inhibitor compounds I [R1 = 4-F, 3,4-di-F, 3,5-di-F; R2 = 2-F, 3-F, 2-Cl, 2,6-di-F, 2,5-di-F, 2-F-6-Cl; R3 = H, Cl, Br; R4 = H, Me, Et] with an improved cutaneous safety property. According to our previous research, compound I [R1 = 3,4-di-F; R2 = R3 = H; R4 = Me] was selected for further optimization for overcoming the disadvantages of compound II, including high Akt2 inhibition and high toxicity against HaCaT keratinocytes. The dihedral angle-based design and mol. dynamics simulation led to the identification of Hu7691 I [R1 = 3,4-di-F; R2 = 2-F; R3 = H; R4 = Me] that achieves a 24-fold selectivity between Akt1 and Akt2. Hu7691 I [R1 = 3,4-di-F; R2 = 2-F; R3 = H; R4 = Me] exhibited low activity in inducing HaCaT apoptosis, promising kinase selectivity, and excellent anticancer cell proliferation potencies. Based on the superior results of safety property, pharmacokinetic profile, and in vivo efficacy, the National Medical Products Administration (NMPA) approved the investigational new drug (IND) application of Hu7691 I [R1 = 3,4-di-F; R2 = 2-F; R3 = H; R4 = Me]. In the part of experimental materials, we found many familiar compounds, such as 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Electric Literature of C9H15BN2O2)

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Electric Literature of C9H15BN2O2

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Recommanded Product: 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleIn 2015 ,《Discovery of potent and selective urea-based ROCK inhibitors: Exploring the inhibitor’s potency and ROCK2/PKA selectivity by 3D-QSAR, molecular docking and molecular dynamics simulations》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Mei, Ding; Yin, Yan; Wu, Fanhong; Cui, Jiaxing; Zhou, Hong; Sun, Guofeng; Jiang, Yu; Feng, Yangbo. The article conveys some information:

An activity model and a selectivity model from 3D-QSAR studies were established by CoMFA and CoMSIA to explore the SAR. Then docking was used to study the binding modes between ligand and kinases (ROCK2 and PKA), and the mol. docking results were further validated by MD simulations. Computational results suggested that substitution containing pos. charge attached to the middle Ph ring, or electropos. group in urea linker was favored for both activity and ROCK2/PKA selectivity. Finally, three compounds were designed, and biol. evaluation demonstrated that these mol. models were effective for guiding the design of potent and selective ROCK inhibitors. The results came from multiple reactions, including the reaction of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Recommanded Product: 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole)

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Recommanded Product: 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

In 2011,Cui, J. Jean; Tran-Dube, Michelle; Shen, Hong; Nambu, Mitchell; Kung, Pei-Pei; Pairish, Mason; Jia, Lei; Meng, Jerry; Funk, Lee; Botrous, Iriny; McTigue, Michele; Grodsky, Neil; Ryan, Kevin; Padrique, Ellen; Alton, Gordon; Timofeevski, Sergei; Yamazaki, Shinji; Li, Qiuhua; Zou, Helen; Christensen, James; Mroczkowski, Barbara; Bender, Steve; Kania, Robert S.; Edwards, Martin P. published 《Structure Based Drug Design of Crizotinib (PF-02341066), a Potent and Selective Dual Inhibitor of Mesenchymal-Epithelial Transition Factor (c-MET) Kinase and Anaplastic Lymphoma Kinase (ALK)》.Journal of Medicinal Chemistry published the findings.Synthetic Route of C9H15BN2O2 The information in the text is summarized as follows:

Because of the critical roles of aberrant signaling in cancer, both c-MET and ALK receptor tyrosine kinases are attractive oncol. targets for therapeutic intervention. The cocrystal structure of 3 (PHA-665752), bound to c-MET kinase domain, revealed a novel ATP site environment, which served as the target to guide parallel, multiattribute drug design. A novel 2-amino-5-aryl-3-benzyloxypyridine series was created to more effectively make the key interactions achieved with 3. In the novel series, the 2-aminopyridine core allowed a 3-benzyloxy group to reach into the same pocket as the 2,6-dichlorophenyl group of 3 via a more direct vector and thus with a better ligand efficiency (LE). Further optimization of the lead series generated the clin. candidate crizotinib (PF-02341066), which demonstrated potent in vitro and in vivo c-MET kinase and ALK inhibition, effective tumor growth inhibition, and good pharmaceutical properties. The experimental part of the paper was very detailed, including the reaction process of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Synthetic Route of C9H15BN2O2)

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) 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. Synthetic Route of C9H15BN2O2

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

In 2022,Wang, Rui-Dong; He, Liancheng; Zhu, Rong-Rong; Jia, Mingxuan; Zhou, Sihan; Tang, Jinsheng; Zhang, Wen-Qian; Du, Lin; Zhao, Qi-Hua published an article in Journal of Hazardous Materials. The title of the article was 《Highly efficient and selective capture Pb(II) through a novel metal-organic framework containing bifunctional groups》.Recommanded Product: 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole The author mentioned the following in the article:

The design and development of materials with a selective adsorption capacity for Pb(II) are very important for environmental governance and ecol. safety. In this work, a novel 3D metal-organic framework ([Cd2H4L4Cl2SO4]·4H2O, Cd-MOF) is constructed using a multiple pyrazole heterocycles tetraphenylethylene-based ligand (H4L4) and CdSO4 which containing Pb(II) adsorption sites (SO42-). Studies have shown that the Cd-MOF has outstanding stability, and its maximum adsorption value of Pb(II) can be as high as 845.55 mg/g, which is higher than that of most MOFs or MOFs modified materials. It is worth emphasizing that the Cd-MOF have excellent recyclability due to the unique adsorption mechanism of the Cd-MOF. Thermodn. studies have shown that Pb(II) adsorption of the Cd-MOF is a spontaneous endothermic process. Specific selective adsorption, exceptional stability and remarkable recyclability make the Cd-MOF a potential material for industrial capture and recovery of Pb(II) from water. In the experimental materials used by the author, we found 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Recommanded Product: 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole)

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Recommanded Product: 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Application of 844501-71-9In 2011 ,《SAR studies of 4-pyridyl heterocyclic anilines that selectively induce autophagic cell death in von Hippel-Lindau-deficient renal cell carcinoma cells》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Bonnet, Muriel; Flanagan, Jack U.; Chan, Denise A.; Lai, Edwin W.; Nguyen, Phuong; Giaccia, Amato J.; Hay, Michael P.. The article conveys some information:

We recently identified a class of pyridyl aniline thiazoles (PAT) that displayed selective cytotoxicity for von Hippel-Lindau (VHL) deficient renal cell carcinoma (RCC) cells in vitro and in vivo. Structure-activity relationship (SAR) studies were used to develop a comparative mol. field anal. (CoMFA) model that related VHL-selective potency to the three-dimensional arrangement of chem. features of the chemotype. We now report the further mol. alignment-guided exploration of the chemotype to discover potent and selective PAT analogs. The contribution of the central thiazole ring was explored using a series of five- and six-membered ring heterocyclic replacements to vary the electronic and steric interactions in the central unit. We also explored a pos. steric CoMFA contour adjacent to the pyridyl ring using Pd-catalyzed cross-coupling Suzuki-Miyaura, Sonogashira and nucleophilic displacement reactions to prepare of a series of aryl-, alkynyl-, alkoxy- and alkylamino-substituted pyridines, resp. In vitro potency and selectivity were determined using paired RCC cell lines: the VHL-null cell line RCC4 and the VHL-pos. cell line RCC4-VHL. Active analogs selectively induced autophagy in RCC4 cells. We have used the new SAR data to further develop the CoMFA model, and compared this to a 2D-QSAR method. Our progress towards realizing the therapeutic potential of this chemotype as a targeted cytotoxic therapy for the treatment of RCC by exploiting the absence of the VHL tumor suppressor gene is reported. The experimental part of the paper was very detailed, including the reaction process of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Application of 844501-71-9)

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Application of 844501-71-9

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

《Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors》 was written by Sharp, Phillip P.; Garnier, Jean-Marc; Hatfaludi, Tamas; Xu, Zhen; Segal, David; Jarman, Kate E.; Jousset, Helene; Garnham, Alexandra; Feutrill, John T.; Cuzzupe, Anthony; Hall, Peter; Taylor, Scott; Walkley, Carl R.; Tyler, Dean; Dawson, Mark A.; Czabotar, Peter; Wilks, Andrew F.; Glaser, Stefan; Huang, David C. S.; Burns, Christopher J.. Recommanded Product: 844501-71-9This research focused ontriazolo benzo diazepine preparation BET domain inhibitor anticancer agent. The article conveys some information:

A number of diazepines are known to inhibit bromo- and extra-terminal domain (BET) proteins. Their BET inhibitory activity derives from the fusion of an acetyl-lysine mimetic heterocycle onto the diazepine framework. Herein we describe a straightforward, modular synthesis of novel 1,2,3-triazolobenzodiazepines and show that the 1,2,3-triazole acts as an effective acetyl-lysine mimetic heterocycle. Structure-based optimization of this series of compounds led to the development of potent BET bromodomain inhibitors, e.g., I, with excellent activity against AF9-MLL-driven leukemic cells, concomitant with a reduction in c-MYC expression. These novel benzodiazepines therefore represent a promising class of therapeutic BET inhibitors.3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Recommanded Product: 844501-71-9) was used in this study.

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Recommanded Product: 844501-71-9

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

In 2016,Crawford, Terry D.; Romero, F. Anthony; Lai, Kwong Wah; Tsui, Vickie; Taylor, Alexander M.; de Leon Boenig, Gladys; Noland, Cameron L.; Murray, Jeremy; Ly, Justin; Choo, Edna F.; Hunsaker, Thomas L.; Chan, Emily W.; Merchant, Mark; Kharbanda, Samir; Gascoigne, Karen E.; Kaufman, Susan; Beresini, Maureen H.; Liao, Jiangpeng; Liu, Wenfeng; Chen, Kevin X.; Chen, Zhongguo; Conery, Andrew R.; Cote, Alexandre; Jayaram, Hariharan; Jiang, Ying; Kiefer, James R.; Kleinheinz, Tracy; Li, Yingjie; Maher, Jonathan; Pardo, Eneida; Poy, Florence; Spillane, Kerry L.; Wang, Fei; Wang, Jian; Wei, Xiaocang; Xu, Zhaowu; Xu, Zhongya; Yen, Ivana; Zawadzke, Laura; Zhu, Xiaoyu; Bellon, Steven; Cummings, Richard; Cochran, Andrea G.; Albrecht, Brian K.; Magnuson, Steven published 《Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300》.Journal of Medicinal Chemistry published the findings.Quality Control of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole The information in the text is summarized as follows:

The single bromodomain of the closely related transcriptional regulators CBP/EP300 is a target of much recent interest in cancer and immune system regulation. A co-crystal structure of a ligand-efficient screening hit and the CBP bromodomain guided initial design targeting the LPF shelf, ZA loop, and acetylated lysine binding regions. Structure-activity relationship studies allowed the authors to identify a more potent analog. Optimization of permeability and microsomal stability and subsequent improvement of mouse hepatocyte stability afforded 59 (GNE-272, TR-FRET IC50 = 0.02 μM, BRET IC50 = 0.41 μM, BRD4(1) IC50 = 13 μM) that retained the best balance of cell potency, selectivity, and in vivo PK. GNE-272 showed a marked antiproliferative effect in hematol. cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model. The results came from multiple reactions, including the reaction of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Quality Control of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole)

3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities. Quality Control of 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics