Tag: M.W=200-250

Hansen, Joshua D. published the artcilePotent and selective pyrazole-based inhibitors of B-Raf kinase, Recommanded Product: 4-(4-Bromo-1H-pyrazol-3-yl)pyridine, the main research area is pyrazole derivative inhibitor B Raf kinase antitumor.

Herein we describe a novel pyrazole-based class of ATP competitive B-Raf inhibitors. These inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. A subset of these inhibitors has demonstrated the ability to inhibit downstream ERK phosphorylation in LOX tumors from mouse xenograft studies.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 166196-54-9 belongs to class pyrazoles-derivatives, name is 4-(4-Bromo-1H-pyrazol-3-yl)pyridine, and the molecular formula is C8H6BrN3, Recommanded Product: 4-(4-Bromo-1H-pyrazol-3-yl)pyridine.

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

Williamson, Alice E. published the artcileOpen Source Drug Discovery: Highly Potent Antimalarial Compounds Derived from the Tres Cantos Arylpyrroles, Quality Control of 217073-76-2, the main research area is arylpyrrole antimalarial malaria.

The development of new antimalarial compounds remains a pivotal part of the strategy for malaria elimination. Recent large-scale phenotypic screens have provided a wealth of potential starting points for hit-to-lead campaigns. One such public set is explored, employing an open source research mechanism in which all data and ideas were shared in real time, anyone was able to participate and patents were not sought. One chem. subseries was found to exhibit oral activity but contained a labile ester that could not be replaced without loss of activity, and the original hit exhibited remarkable sensitivity to minor structural change. A second subseries displayed high potency, including activity within gametocyte and liver stage assays, but at the cost of low solubility As an open source research project, unexplored avenues are clearly identified and may be explored further by the community; new findings may be cumulatively added to the present work.

ACS Central Science published new progress about Antimalarials. 217073-76-2 belongs to class pyrazoles-derivatives, name is 1-(4-Fluorophenyl)-5-methyl-1H-pyrazole-4-carboxylic acid, and the molecular formula is C11H9FN2O2, Quality Control of 217073-76-2.

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

Lesniak, Robert K. published the artcileDiscovery of 1H-Pyrazole Biaryl Sulfonamides as Novel G2019S-LRRK2 Kinase Inhibitors, Recommanded Product: 4-(4-Bromo-1H-pyrazol-3-yl)pyridine, the main research area is pyrazole biaryl sulfonamides preparation G2019S LRRK2 kinase inhibitor.

G2019S (GS) is the most prevalent mutation in the leucine rich repeat protein kinase 2 gene (LRRK2), a genetic predisposition that is common for Parkinson’s disease, as well as for some forms of cancer, and is a shared risk allele for Crohn’s disease. GS-LRRK2 has a hyperactive kinase, and although numerous drug discovery programs have targeted LRRK2 kinase, few have reached clin. development. We report the discovery and preliminary development of an entirely novel structural class of potent and selective GS-LRRK2 kinase inhibitors: biaryl-1H-pyrazoles.

ACS Medicinal Chemistry Letters published new progress about Crohn disease. 166196-54-9 belongs to class pyrazoles-derivatives, name is 4-(4-Bromo-1H-pyrazol-3-yl)pyridine, and the molecular formula is C8H6BrN3, Recommanded Product: 4-(4-Bromo-1H-pyrazol-3-yl)pyridine.

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

Khonde, Lutete Peguy published the artcile1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis, Application In Synthesis of 166196-54-9, the main research area is diarylpyrazolyl acylsulfonamide preparation antituberculosis activity.

Phenotypic whole cell high-throughput screening of a ~150,000 diverse set of compounds against Mycobacterium tuberculosis (Mtb) in cholesterol-containing media identified 1,3-diarylpyrazolyl-acylsulfonamide I as a moderately active hit. Structure-activity relationship (SAR) studies demonstrated a clear scope to improve whole cell potency to MIC values of <0.5μM, and a plausible pharmacophore model was developed to describe the chem. space of active compounds Compounds are bactericidal in vitro against replicating Mtb and retained activity against multidrug-resistant clin. isolates. Initial biol. triage assays indicated cell wall biosynthesis as a plausible mode-of-action for the series. However, no cross-resistance with known cell wall targets such as MmpL3, DprE1, InhA, and EthA was detected, suggesting a potentially novel mode-of-action or inhibition. The in vitro and in vivo drug metabolism and pharmacokinetics profiles of several active compounds from the series were established leading to the identification of a compound for in vivo efficacy proof-of-concept studies. Journal of Medicinal Chemistry published new progress about Homo sapiens. 166196-54-9 belongs to class pyrazoles-derivatives, name is 4-(4-Bromo-1H-pyrazol-3-yl)pyridine, and the molecular formula is C8H6BrN3, Application In Synthesis of 166196-54-9.

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

Yan, Bing published the artcileStructure-Dependent Response of a Chemiluminescence Nitrogen Detector for Organic Compounds with Adjacent Nitrogen Atoms Connected by a Single Bond, Safety of 1-(4-Fluorophenyl)-5-methyl-1H-pyrazole-4-carboxylic acid, the main research area is HPLC chemiluminescence nitrogen detector structure dependent response; single bond connected adjacent nitrogen atom organic compound detector; pyrazole hydrazine triazole derivative HPLC chemiluminescence nitrogen detector; high throughput screening pyrazole hydrazine triazole derivative chemiluminescence detector.

High-throughput screening (HTS) of chem. libraries is indispensable for drug discovery research. However, the HTS data quality for lead discovery, lead optimization, and quant. structure activity relation studies was severely compromised due to the uncertain compound concentrations in screening plates. To address this issue, the authors compared various high-throughput technologies for quantification of compounds in microtiter plate format without the need for authentic compounds as standards and identified the chemiluminescence nitrogen detector (CLND) as the method of choice at the present time. However, the structure dependence of this detector was not well studied. A proposed rule suggested that the only exception to equimolar response is for compounds that contain adjacent nitrogen atoms. The response should be zero when the adjacent nitrogen atoms are connected by a double bond and 0.5 when they are connected by a single bond. The authors studied a broad range of compounds with isolated and adjacent nitrogen atoms. Compounds with isolated nitrogen atoms produce an equimolar response with a 15-20% variation depending on structures and compounds with adjacent nitrogen atoms connected by a double bond giving nearly zero response. The CLND response for compounds containing adjacent nitrogen atoms that are connected with a single bond is highly structure dependent. Substitutions on the nitrogen atoms or nearby in the mol. can increase the CLND response to approach a value higher than the predicted value 0.5 (maximal value 0.82/nitrogen atom). Without substitution, much lower values than predicted (minimal value 0.0-0.08/nitrogen atom) were obtained. Therefore, the prediction of response of 0.5/nitrogen atom for compounds with adjacent nitrogen atoms connected by a single bond should be abandoned. Compounds with similar structures should be used to generate calibration curves for quantification of this class of compounds

Analytical Chemistry published new progress about Chemiluminescence. 217073-76-2 belongs to class pyrazoles-derivatives, name is 1-(4-Fluorophenyl)-5-methyl-1H-pyrazole-4-carboxylic acid, and the molecular formula is C11H9FN2O2, Safety of 1-(4-Fluorophenyl)-5-methyl-1H-pyrazole-4-carboxylic acid.

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

Wang, Alan X. published the artcileSynthesis and immunosuppressant activity of pyrazolecarboxamides, Quality Control of 217073-76-2, the main research area is pyrazolecarboxamide derivative preparation immunosuppressant activity.

A series of novel pyrazolecarboxamides, e.g., I, is disclosed that demonstrate strong immunosuppressant activity in rodent and human mixed leukocyte response (MLR) assays (IC50 <1 μM). The synthesis, biol. activity, mode of action, and pharmacokinetic properties of this new lead series are discussed. Bioorganic & Medicinal Chemistry Letters published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 217073-76-2 belongs to class pyrazoles-derivatives, name is 1-(4-Fluorophenyl)-5-methyl-1H-pyrazole-4-carboxylic acid, and the molecular formula is C11H9FN2O2, Quality Control of 217073-76-2.

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

Pyrazoles are synthesized by the reaction of α,β-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine (Knorr-type reactions). For example, acetylacetone and hydrazine gives 3,5-dimethylpyrazole. Application In Synthesis of 761446-44-0.

Zhang, Yun;Xia, Anjie;Zhang, Shiyu;Lin, Guifeng;Liu, Jingming;Chen, Pei;Mu, Bo;Jiao, Yan;Xu, Wenwen;Chen, Mingxin;Li, Linli research published 《 Discovery of 3,6-disubstituted-imidazo[1,2-a]pyridine derivatives as a new class of CLK1 inhibitors》, the research content is summarized as follows. Inhibition of cdc2-like kinase1 (CLK1) could efficiently induce autophagy and it has been thought as a potential target for treatment of autophagy-related diseases. Herein we report the discovery of a series of 3,6-disubstituted-imidazo[1,2-a]pyridine derivatives as a new class of CLK1 inhibitors. Among them, compound 9e (I) is the most potent one, which exhibits an IC₅₀ value of 4 nM against CLK1 kinase. In vitro, this compound reduces the phosphorylation level of the typical downstream substrates of CLK1 and affects their subcellular redistribution. Further study indicates that 9e is efficient to induce autophagy. Overall, this study provides a promising lead compound for drug discovery targeting CLK1 kinase.

Application In Synthesis of 761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., 761446-44-0.

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

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. Name: 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole.

Zhong, Zhenpeng;Shi, Liyang;Fu, Tiancheng;Huang, Jiajun;Pan, Zhengying research published 《 Discovery of Novel 7-Azaindole Derivatives as Selective Covalent Fibroblast Growth Factor Receptor 4 Inhibitors for the Treatment of Hepatocellular Carcinoma》, the research content is summarized as follows. Fibroblast growth factor receptor 4 (FGFR4) has been identified as a potential target for the treatment of hepatocellular carcinoma (HCC) with aberrant FGFR4 signaling because of its important role in HCC progression and development. Several FGFR4 inhibitors are under clin. development. Using a 7-azaindole scaffold, we discovered a series of novel selective and covalent FGFR4 inhibitors by performing a structure-based design approach. Representative compounds I and II exhibited potent FGFR4 inhibition and high selectivity among kinases. Western blot anal. showed that compounds I and II significantly inhibited the FGF19/FGFR4 signaling pathway in HuH-7 cells and effectively suppressed the proliferation of HuH-7 HCC cells and MDA-MB-453 breast cancer cells. Moreover, compound II exhibited significant in vivo antitumor activity in a mouse HuH-7 xenograft model. Thus, compound II and the 7-azaindole scaffold can be applied to develop anticancer agents for the treatment of cancers characterized by aberrant FGFR4 signaling.

761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., Name: 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

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

Pyrazole is an organic compound with the formula C3H3N2H. It is a heterocycle characterized by a 5-membered ring of three carbon atoms and two adjacent nitrogen atoms, which are in ortho-substitution. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Pyrazoles are a class of compounds that have the ring C3N2 with adjacent nitrogen atoms.Notable drugs containing a pyrazole ring are celecoxib (celebrex) and the anabolic steroid stanozolol. Safety of 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole.

Zhou, Hua;McGowan, Meredeth A.;Lipford, Kathryn;Christopher, Matthew;Fradera, Xavier;Witter, David;Lesburg, Charles A.;Li, Chaomin;Methot, Joey L.;Lampe, John;Achab, Abdelghani;Shaffer, Lynsey;Goldenblatt, Peter;Shah, Sanjiv;Bass, Alan;Schroeder, Gottfried;Chen, Dapeng;Zeng, Haoyu;Augustin, Martin A.;Katz, Jason D. research published 《 Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors》, the research content is summarized as follows. A high-throughput screening (HTS) campaign identified a class of heteroaryl piperazines with excellent baseline affinity and selectivity for phosphoinositide 3-kinase δ (PI3Kδ) over closely related isoforms. Rapid evaluation and optimization of structure-activity relationships (SAR) for this class, leveraging the modular nature of this scaffold, facilitated development of this hit class into a series of potent and selective inhibitors of PI3Kδ. This effort culminated in the identification of 29, which displayed excellent potency in enzyme and cell-based assays, as well as favorable pharmacokinetic and off-target profiles.

761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., Safety of 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole

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

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 °C).Pyrazole used as a ligand to prepare organometallic compounds. COA of Formula: C10H17BN2O2.

Zhuo, Lin-Sheng;Wang, Ming-Shu;Wu, Feng-Xu;Xu, Hong-Chuang;Gong, Yi;Yu, Zhi-Cheng;Tian, Yan-Guang;Pang, Chao;Hao, Ge-Fei;Huang, Wei;Yang, Guang-Fu research published 《 Discovery of Next-Generation Tropomyosin Receptor Kinase Inhibitors for Combating Multiple Resistance Associated with Protein Mutation》, the research content is summarized as follows. Tropomyosin receptor kinase (TRK) inhibition is an effective therapeutic approach for treatment of a variety of cancers. Despite the use of first-generation TRK inhibitor (TRKI) larotrectinib (1) resulting in significant therapeutic response in patients, acquired resistance develops invariably. The emergence of secondary mutations occurring at the solvent-front, xDFG, and gatekeeper regions of TRK represents a common mechanism for acquired resistance. However, xDFG mutations remain insensitive to second-generation macrocyclic TRKIs selitrectinib (3) and repotrectinib (4) designed to overcome the resistance mediated by solvent-front and gatekeeper mutations. Here, we report the structure-based drug design and discovery of a next-generation TRKI. The structure-activity relationship studies culminated in the identification of a promising drug candidate 8 that showed excellent in vitro potency on a panel of TRK mutants, especially TRKA^G667C in the xDFG motif, and improved in vivo efficacy than 1 and 3 in TRK wild-type and mutant fusion-driven tumor xenograft models, resp.

761446-44-0, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g/mol. The purity is usually 95%., COA of Formula: C10H17BN2O2

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