Category: 837392-67-3

Quality Control of tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate, is researched, Molecular C19H28BNO4, CAS is 837392-67-3, about Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).

Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states. Evidence that PERK is implicated in tumorigenesis and cancer cell survival stimulated our search for small mol. inhibitors. Through screening and lead optimization using the human PERK crystal structure, we discovered compound I (GSK2606414), an orally available, potent, and selective PERK inhibitor. Compound I inhibits PERK activation in cells and inhibits the growth of a human tumor xenograft in mice.

Different reactions of this compound(tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate)Quality Control of tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate require different conditions, so the reaction conditions are very important.

Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Quality Control of tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate, is researched, Molecular C19H28BNO4, CAS is 837392-67-3, about Discovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK).

Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states. Evidence that PERK is implicated in tumorigenesis and cancer cell survival stimulated our search for small mol. inhibitors. Through screening and lead optimization using the human PERK crystal structure, we discovered compound I (GSK2606414), an orally available, potent, and selective PERK inhibitor. Compound I inhibits PERK activation in cells and inhibits the growth of a human tumor xenograft in mice.

Different reactions of this compound(tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate)Quality Control of tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate require different conditions, so the reaction conditions are very important.

Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 837392-67-3, is researched, Molecular C19H28BNO4, about Synthesis and Pharmacological Evaluation of Noncatechol G Protein Biased and Unbiased Dopamine D1 Receptor Agonists, the main research direction is noncatechol G protein biased unbiased dopamine D1 receptor preparation.Product Details of 837392-67-3.

Noncatechol heterocycles have recently been discovered as potent and selective G protein biased dopamine 1 receptor (D1R) agonists with superior pharmacokinetic properties. To determine the structure-activity relations centered on G protein or β-arrestin signaling bias, systematic medicinal chem. was employed around three aromatic pharmacophores of the lead compound PF2334, generating a series of new mols. that were evaluated at both D1R Gs-dependent cAMP signaling and β-arrestin recruitment in HEK293 cells. Here, the authors report the chem. synthesis, pharmacol. evaluation, and mol. docking studies leading to the identification of two novel noncatechol D1R agonists that are a subnanomolar potent unbiased ligand 6-(4-(Furo[3,2-c]pyridin-4-yloxy)-2-methylphenyl)-1,5-dimethylpyrimidine-2,4(1H,3H)dione (PW0441) and a nanomolar potent complete G protein biased ligand 6-(4-((3-(Difluoromethoxy)pyridin-2-yl)oxy)-2-methylphenyl)-1,5-dimethylpyrimidine-2,4(1H,3H)-dione (PW0464), resp. These novel D1R agonists provide important tools to study D1R activation and signaling bias in both health and disease.

Although many compounds look similar to this compound(837392-67-3)Product Details of 837392-67-3, numerous studies have shown that this compound(SMILES:O=C(N1CCC2=C1C=CC(B3OC(C)(C)C(C)(C)O3)=C2)OC(C)(C)C), has unique advantages. If you want to know more about similar compounds, you can read my other articles.

Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 837392-67-3, is researched, SMILESS is O=C(N1CCC2=C1C=CC(B3OC(C)(C)C(C)(C)O3)=C2)OC(C)(C)C, Molecular C19H28BNO4Journal, Article, Research Support, Non-U.S. Gov’t, Journal of Medicinal Chemistry called Insights of a Lead Optimization Study and Biological Evaluation of Novel 4-Hydroxytamoxifen Analogs as Estrogen-Related Receptor γ (ERRγ) Inverse Agonists, Author is Kim, Jina; Woo, Seo Yeon; Im, Chun Young; Yoo, Eun Kyung; Lee, Seungmi; Kim, Hyo-Ji; Hwang, Hee-Jong; Cho, Joong-heui; Lee, Won Seok; Yoon, Heeseok; Kim, Shinae; Kwon, Oh-bin; Hwang, Hayoung; Kim, Kyung-Hee; Jeon, Jae-Han; Singh, Thoudam Debraj; Kim, Sang Wook; Hwang, Sung Yeoun; Choi, Hueng-Sik; Lee, In-Kyu; Kim, Seong Heon; Jeon, Yong Hyun; Chin, Jungwook; Cho, Sung Jin, the main research direction is hydroxytamoxifen analog synthesis SAR cytotoxicity pharmacokinetics estrogen related receptor.Name: tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate.

We evaluated the in vitro pharmacol. as well as the absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties of chem. entities that have not only shown to be highly selective agonists for ERRγ, but also exhibited enhanced pharmacokinetic profile than 3 (GSK5182). 6G and 10b had comparable potency to 3 and were far more selective for ERRγ over the ERRα, -β, and ERα. The in vivo pharmacokinetic profiles of 6g and 10b were further evaluated as they possessed superior in vitro ADMET profiles compared to the other compounds Addnl., we observed a significant increase of fully-glycosylated NIS protein, key protein for radioiodine therapy in anaplastic thyroid cancer (ATC), in 6g- or 10b-treated CAL62 cells, which indicated that these compounds could be promising enhancers for restoring NIS protein function in ATC cells. Thus, 6g and 10b possess advantageous drug-like properties and can be used to potentially treat various ERRγ-related disorders.

Compounds in my other articles are similar to this one(tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate)Name: tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate, you can compare them to see their pros and cons in some ways,such as convenient, effective and so on.

Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Quality Control of tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate, is researched, Molecular C19H28BNO4, CAS is 837392-67-3, about Chan-Evans-Lam Amination of Boronic Acid Pinacol (BPin) Esters: Overcoming the Aryl Amine Problem. Author is Vantourout, Julien C.; Law, Robert P.; Isidro-Llobet, Albert; Atkinson, Stephen J.; Watson, Allan J. B..

The Chan-Evans-Lam reaction is a valuable C-N bond forming process. However, aryl boronic acid pinacol (BPin) ester reagents can be difficult coupling partners that often deliver low yields, in particular in reactions with aryl amines. Herein, we report effective reaction conditions for the Chan-Evans-Lam amination of aryl BPin with alkyl and aryl amines. A mixed MeCN/EtOH solvent system was found to enable effective C-N bond formation using aryl amines while EtOH is not required for the coupling of alkyl amines.

In some applications, this compound(837392-67-3)Quality Control of tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate is unique.If you want to know more details about this compound, you can contact with the author or consult more relevant literature.

Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 837392-67-3, is researched, Molecular C19H28BNO4, about Optimization of drug candidates that inhibit the D-loop activity of RAD51, the main research direction is RAD51 D loop homologous recombination quinoxaline; DNA repair; biological activity; cancer; inhibitors; structure-activity relationships.Product Details of 837392-67-3.

RAD51 is the central protein in homologous recombination (HR) repair, where it first binds ssDNA and then catalyzes strand invasion via a D-loop intermediate. Addnl., RAD51 plays a role in faithful DNA replication by protecting stalled replication forks; this requires RAD51 to bind DNA but may not require the strand invasion activity of RAD51. We previously described a small-mol. inhibitor of RAD51 named RI(dl)-2 (RAD51 inhibitor of D-loop formation #2, hereafter called 2h(I)), which inhibits D-loop activity while sparing ssDNA binding. However, I is limited in its ability to inhibit HR in vivo, preventing only about 50 % of total HR events in cells. We sought to improve upon this by performing a structure-activity relationship (SAR) campaign for more potent analogs of I. Most compounds were prepared from 1-(2-aminophenyl)pyrroles by forming the quinoxaline moiety either by condensation with aldehydes, then dehydrogenation of the resulting 4,5-dihydro intermediates, or by condensation with N,N’-carbonyldiimidazole, chlorination, and installation of the 4-substituent through Suzuki-Miyaura coupling. Many analogs exhibited enhanced activity against human RAD51, but in several of these compounds the increased inhibition was due to the introduction of dsDNA intercalation activity. We developed a sensitive assay to measure dsDNA intercalation, and identified two analogs of I that promote complete HR inhibition in cells while exerting minimal intercalation activity.

There are many compounds similar to this compound(837392-67-3)Product Details of 837392-67-3. if you want to know more, you can check out my other articles. I hope it will help you，maybe you’ll find some useful information.

Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Quality Control of tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate, is researched, Molecular C19H28BNO4, CAS is 837392-67-3, about Identification of 5-(2,3-Dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as a new class of receptor-interacting protein kinase 1 (RIPK1) inhibitors, which showed potent activity in a tumor metastasis model. Author is Li, Yueshan; Xiong, Yu; Zhang, Guo; Zhang, Liting; Yang, Wei; Yang, Jiao; Huang, Luyi; Qiao, Zeen; Miao, Zhuang; Lin, Guifeng; Sun, Qiu; Niu, Ting; Chen, Lijuan; Niu, Dawen; Li, Linli; Yang, Shengyong.

We herein report the structural optimization and structure-activity relationship studies of 5-(2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as a new class of receptor-interacting protein kinase 1 (RIPK1) inhibitors. Among all obtained RIPK1 inhibitors, I is the most active one. This compound potently inhibited RIPK1 with a binding affinity (KD) of 0.004μM and an enzymic IC50 value of 0.011μM and also showed good kinase selectivity. It could efficiently protect cells from necroptosis and attenuate the necrotic cell death of vascular endothelial cells induced by tumor cells both in vitro and in vivo. Importantly, I exhibited excellent antimetastasis activity in the exptl. B16 melanoma lung metastasis model. It also displayed favorable pharmacokinetic properties. Collectively, I could be a promising agent for preventing tumor metastasis.

I hope my short article helps more people learn about this compound(tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate)Quality Control of tert-Butyl 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)indoline-1-carboxylate. Apart from the compound(837392-67-3), you can read my other articles to know other related compounds.

Reference:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics