Category: 118430-74-3

Zhang, Juan; Li, Xianfeng; Wei, Haimei; Li, Yangfeng; Zhang, Gong; Li, Yizhou published the artcile< Sequential DNA-Encoded Building Block Fusion for the Construction of Polysubstituted Pyrazoline Core Libraries>, Application of C7H11N3, the main research area is aryl amine DNA encoded aldehyde cyclization; encoded DNA tetrazole preparation alkene cycloaddition; DNA encoded pyrazoline preparation.

Herein, a sequential DNA-encoded synthesis strategy for polysubstituted pyrazoline heterocycles, which fuses a broad panel of aldehydes, aryl amines, and alkenes as building blocks was reported. Furthermore, mock library synthesis and selection demonstrated the ability of the method to produce DNA-encoded focused libraries with highly functionalized pyrazoline cores.

Organic Letters published new progress about 1,3-Dipolar cycloaddition reaction. 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, Application of C7H11N3.

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

Jiang, Bo; Ning, Yi; Fan, Wei; Tu, Shu-Jiang; Li, Guigen published the artcile< Oxidative Dehydrogenative Couplings of Pyrazol-5-amines Selectively Forming Azopyrroles>, Quality Control of 118430-74-3, the main research area is stereoselective synthesis azopyrrole; oxidative dehydrogenative coupling pyrazolamine copper iodine.

New oxidative dehydrogenative couplings of pyrazol-5-amines for the selective synthesis of azopyrrole derivatives have been described. The reaction simultaneously installs C-I and N-N bonds through iodination and oxidation; a copper-catalyzed oxidative coupling process led to azopyrroles,. E.g., in presence of I2, TBHP, and K2CO3 in EtOH, dehydrogenative coupling of pyrazol-5-amine (I) gave 86% iodinated azopyrrole [(E)-II]. E.g., in presence of CuI, 1,10-phenanthroline, and TBHP in CH2Cl2, dehydrogenative coupling of I gave 56% (E)-III. The resulting iodo-substituted azopyrroles were employed by treatment with various terminal alkynes through Sonogashira cross-coupling leading to new azo compounds

Journal of Organic Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, Quality Control of 118430-74-3.

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

Zhao, Yujun; Zhou, Bing; Bai, Longchuan; Liu, Liu; Yang, Chao-Yie; Meagher, Jennifer L.; Stuckey, Jeanne A.; McEachern, Donna; Przybranowski, Sally; Wang, Mi; Ran, Xu; Aguilar, Angelo; Hu, Yang; Kampf, Jeff W.; Li, Xiaoqin; Zhao, Ting; Li, Siwei; Wen, Bo; Sun, Duxin; Wang, Shaomeng published the artcile< Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor>, Synthetic Route of 118430-74-3, the main research area is pyrazole pyrimido indole preparation bromodomain inhibitor cancer.

We report the structure-based discovery of CF53 (28) as a highly potent and orally active inhibitor of bromodomain and extra-terminal (BET) proteins. By the incorporation of a NH-pyrazole group into the 9H-pyrimido[4,5-b]indole core, we identified a series of compounds that bind to BRD4 BD1 protein with Ki values of <1 nM and achieve low nanomolar potencies in the cell growth inhibition of leukemia and breast cancer cells. The most-promising compound, CF53, possesses excellent oral pharmacokinetic properties and achieves significant antitumor activity in both triple-neg. breast cancer and acute leukemia xenograft models in mice. Determination of the co-crystal structure of CF53 with the BRD4 BD1 protein provides a structural basis for its high binding affinity to BET proteins. CF53 is very selective over non-BET bromodomain-containing proteins. These data establish CF53 as a potent, selective, and orally active BET inhibitor, which warrants further evaluation for advanced preclin. development. Journal of Medicinal Chemistry published new progress about Antitumor agents. 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, Synthetic Route of 118430-74-3.

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

Morgentin, Remy; Barlaam, Bernard; Foote, Kevin; Hassall, Lorraine; Hawkins, Janet; Jones, Clifford D.; Le Griffon, Antoine; Peru, Aurelien; Ple, Patrick published the artcile< Two-Directional Approach for the Rapid Synthesis of 2,4-Bis-Aminoaryl Pyridine Derivatives>, Electric Literature of 118430-74-3, the main research area is aminoarylpyridine preparation coupling palladium; pyridine aminoaryl preparation coupling palladium; Buchwald Hartwig regioselective nucleophilic substitution bisaminoarylpyridine preparation.

We have developed two different approaches in parallel to rapidly access 2,4-bis(aminoaryl)pyridine compounds, e.g., I, from a common starting material. The C-4/C-2 approach uses palladium-mediated coupling reactions to sequentially functionalize C-4 and then C-2. An alternative C-2/C-4 route uses a regioselective SNAr reaction to first substitute at C-2 then subsequently at C-4 by a palladium-mediated reaction. Both approaches have been used successfully to provide a range of 2,4-bis(aminoaryl)pyridine compounds

Synthetic Communications published new progress about Buchwald-Hartwig reaction. 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, Electric Literature of 118430-74-3.

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

Saha, Debasmita; Ryan, Katie Rose; Lakkaniga, Naga Rajiv; Smith, Erica Lane; Frett, Brendan published the artcile< Pyrazoloadenine Inhibitors of the RET Lung Cancer Oncoprotein Discovered by a Fragment Optimization Approach>, Safety of 3-Cyclopropyl-1-methyl-1H-pyrazol-5-amine, the main research area is pyrazoloadenine inhibitor RET lung cancer oncoprotein fragment optimization; RET inhibitor; fragment-based drug discovery; oncoproteins; pyrazoloadenines.

A fragment-based drug-discovery approach was used on a pyrazoloadenine fragment library to uncover new mols. that target the RET (REarranged during Transfection) oncoprotein, which is a driver oncoprotein in ∼2 % of non-small-cell lung cancers. The fragment library was screened against the RET kinase and LC-2/ad (RET-driven), KM-12 (TRKA-driven matched control) and A549 (cytotoxic control) cells to identify selective scaffolds that could inhibit RET-driven growth. An unsubstituted pyrazoloadenine fragment was found to be active on RET in a biochem. assay, but reduced cell viability in non-RET-driven cell lines (EC50=1 and 3 μM, resp.). To increase selectivity for RET, the pyrazoloadenine was modeled in the RET active site, and two domains were identified that were probed with pyrazoloadenine fragment derivatives to improve RET affinity. Scaffolds at each domain were merged to generate a novel lead compound, 8 p (I), which exhibited improved activity and selectivity for the RET oncoprotein (A549 EC50=5.92 μM, LC-2/ad EC50=0.016 μM, RET IC50=0.000326 μM).

ChemMedChem published new progress about Antitumor agents. 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, Safety of 3-Cyclopropyl-1-methyl-1H-pyrazol-5-amine.

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

Zhang, Shiyan; Huang, Chaoying; Lyu, Xilin; Wang, Peipei; Zang, Yi; Wang, Zengtao; Wang, Huan; Li, Jia; Zhao, Yujun published the artcile< Discovery of a 2-pyridinyl urea-containing compound YD57 as a potent inhibitor of apoptosis signal-regulating kinase 1 (ASK1)>, Name: 3-Cyclopropyl-1-methyl-1H-pyrazol-5-amine, the main research area is pyridinyl urea containing compound preparation ASK1 inhibitor cancer; ASK1; ASK2; Apoptosis; Cell cycle arrest; Selectivity.

Inhibition of MAP3K kinase ASK1 has been an attractive strategy for the treatment of nonalcoholic steatohepatitis and multiple sclerosis, among others. Herein, we reported the discovery of 2-pyridinyl urea-containing compound 14l (YD57) as a potent, small-mol. inhibitor of ASK1. 14l was selective against MAP3K kinases ASK2 and TAK1 (>140-fold), while it also inhibited several cell cycle regulating kinases with IC50 values in a range of 90-400 nM (<20-fold selectivity). As a consequence, 14l had stronger apoptosis induction, more potent G1 cell cycle arrest activities, and lower IC50 value of cell growth inhibition than that of GS4997 in HepG2 cancer cell line. On the other hand, 14l did not inhibit ASK1 and p38 phosphorylation in intact cells. We reason that the multi-target effects of 14l likely neutralized the activities caused by inhibition of cellular ASK1. Future studies of these ASK1 inhibitors should pay close attention to their kinome selectivity profile. European Journal of Medicinal Chemistry published new progress about Antitumor agents. 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, Name: 3-Cyclopropyl-1-methyl-1H-pyrazol-5-amine.

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

Kokorekin, Vladimir A.; Sigacheva, Vera L.; Petrosyan, Vladimir A. published the artcile< New data on heteroarene thiocyanation by anodic oxidation of NH4SCN. The processes of electroinduced nucleophilic aromatic substitution of hydrogen>, COA of Formula: C7H11N3, the main research area is heteroarene thiocyanation anodic oxidation ammonium thiocyanate.

Potentiostatic (galvanostatic) electrolysis of NH4SCN in an undivided cell under mild conditions (25 °C, Pt anode, MeCN) was employed to perform the anodic thiocyanation of nitrogen-containing heterocycles with yields up to 95%. The regularities of the process are discussed, which show that it can be considered as electroinduced nucleophilic aromatic substitution of hydrogen.

Tetrahedron Letters published new progress about Cyanation, thiocyanation. 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, COA of Formula: C7H11N3.

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

Lyalin, Boris V.; Sigacheva, Vera L.; Kokorekin, Vladimir A.; Petrosyan, Vladimir A. published the artcile< A new synthesis of azopyrazoles by oxidation of C-aminopyrazoles on a NiO(OH) electrode>, Application of C7H11N3, the main research area is amino pyrazole electrochem oxidation; azopyrazole diastereoselective preparation.

Oxidation of C-amino-N-alkylpyrazoles on a NiO(OH) electrode in an aqueous alk. medium afforded the corresponding azopyrazoles. The success in implementation of these processes was due to the structure of C-aminopyrazoles.

Mendeleev Communications published new progress about Azo compounds Role: SPN (Synthetic Preparation), PREP (Preparation). 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, Application of C7H11N3.

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

Adachi, Ikuo; Yamamori, Teruo; Hiramatsu, Yoshiharu; Sakai, Katsunori; Sato, Hatsuo; Kawakami, Masaru; Uno, Osamu; Ueda, Motohiko published the artcile< Studies on dihydropyridines. II. Synthesis of 4,7-dihydropyrazolo[3,4-b]pyridines with vasodilating and antihypertensive activities>, Formula: C7H11N3, the main research area is coronary vasodilator dihydropyrazolopyridine preparation; structure property relationship dihydropyrazolopyridine antihypertensive; pyrazolopyridine dihydro antihypertensive preparation; aminopyrazole unsaturated ketoester cyclocondensation; calcium channel blocker dihydropyrazolopyridine.

A series of 4-aryl-4,7-dihydropyrazolo[3,4-b]pyridine-5-carboxylate derivatives I (R = Me, Ph, cyclopentyl; R1 = Me, Et, CHMe2, cyclohexyl, substituted phenethyl, etc.; R2 = 2-O2NC6H4, 3-O2NC6H4, 2-ClC6H4, 2.8-Cl2C6H4, pyridyl; R3 = H, Me, CHMe2, Ph, cycloalkyl, CO2Et, pyridyl, etc.) was prepared and the compounds were tested for Ca-blocking activity in isolated guinea pig portal vein, antihypertensive activity in spontaneously hypertensive rats, and coronary vasodilating effect in isolated guinea pig heart. A number of derivatives had potent antihypertensive and coronary vasodilating activities. The structure-activity relationships of the series indicated that a 3-cyclopentyl or 3-cyclohexyl substituent and a hydrophobic 5-ester moiety with moderate bulkiness were effective for increasing the pharmacol. potencies.

Chemical & Pharmaceutical Bulletin published new progress about Antihypertensives. 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, Formula: C7H11N3.

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

Xun, Zhan; Feng, Xian; Wang, Jianjun; Shi, Daqing; Huang, Zhibin published the artcile< Multicomponent Strategy for the Preparation of Pyrrolo[1,2-a]pyrimidine Derivatives under Catalyst-Free and Microwave Irradiation Conditions>, Name: 3-Cyclopropyl-1-methyl-1H-pyrazol-5-amine, the main research area is pyrrolopyrimidine preparation microwave irradiation regioselective; aminopyrazole acetylenedicarboxylate malononitrile multicomponent reaction.

A simple and efficient one-pot procedure has been developed for the construction of pyrrolo[1,2-a]pyrimidines I (R = Me, Et; R1 = H, CH3, C6H5; R2 = Me, Ph, cyclopropyl) via the three-component domino reaction of 5-aminopyrazoles II, acetylenedicarboxylates RCO2CCCO2R and malononitrile under catalyst-free, microwave irradiation conditions. The key step in this transformation is the N-N bond cleavage reaction of the II substrate, which has been reported in this context for the first time in this study. The advantages of this protocol include readily available starting materials, short reaction times and good regioselectivity.

Chinese Journal of Chemistry published new progress about Microwave irradiation. 118430-74-3 belongs to class pyrazoles-derivatives, and the molecular formula is C7H11N3, Name: 3-Cyclopropyl-1-methyl-1H-pyrazol-5-amine.

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