Tag: M.W=100-150

Abebe, Felagot A. published the artcileDevelopment of a Rapid In Vitro Screening Assay Using Metabolic Inhibitors to Detect Highly Selective Anticancer Agents, Application of 2-Methoxynicotinaldehyde, the main research area is antitumor drug screening assay metabolic inhibitor.

Traditional long exposure (24-72 h) cell viability assays for identification of potential drug compounds can fail to identify compounds that are: (a) biol. active but not toxic and (b) inactive without the addition of a synergistic additive. Herein, we report the development of a rapid (1-2 h) compound screening technique using a com. available cell viability kit (CellTiter-Glo) that has led to the detection of compounds that were not identified as active agents using traditional cytotoxicity screening methods. These compounds, in combination with metabolic inhibitor 2-deoxyglucose, display selectivity toward a pancreatic cancer cell line. An evaluation of 11 mammalian cell lines against 30 novel compounds and two metabolic inhibitors is reported. The inclusion of metabolic inhibitors during an initial screening process, and not simply during mechanistic investigations of a previously identified hit compound, provides a rapid and sensitive tool for identifying drug candidates potentially overlooked by other methods.

ACS Omega published new progress about Antitumor agents. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Application of 2-Methoxynicotinaldehyde.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Schroeder, Gretchen M. published the artcileDiscovery of N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficacious Inhibitor of the Met Kinase Superfamily, Application In Synthesis of 71255-09-9, the main research area is aminopyridinyloxy fluorophenyl dihydropyridine carboxamide preparation Met kinase inhibitor.

Substituted N-(4-(2-aminopyridin-4-yloxy)-3-fluoro-phenyl)-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamides were identified as potent and selective Met kinase inhibitors. Substitution of the pyridine 3-position gave improved enzyme potency, while substitution of the pyridone 4-position led to improved aqueous solubility and kinase selectivity. Analog 10 demonstrated complete tumor stasis in a Met-dependent GTL-16 human gastric carcinoma xenograft model following oral administration. Because of its excellent in vivo efficacy and favorable pharmacokinetic and preclin. safety profiles, 10 has been advanced into phase I clin. trials.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Application In Synthesis of 71255-09-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Krishnaiah, Maddeboina published the artcileSynthesis and biological evaluation of 5-(fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles as inhibitors of transforming growth factor-β type I receptor kinase, Name: [1,2,4]Triazolo[1,5-a]pyridine-6-carbaldehyde, the main research area is triazolopyridinylimidazole pyridinyl preparation transforming growth factor kinase inhibitor; ALK5 inhibitor; Cancer; Fibrosis; Kinase assay; TGF-β.

To further optimize a clin. candidate (EW-7197), a series of 5-(3-, 4-, or 5-fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles have been synthesized and evaluated for their TGF-β type I receptor kinase (ALK5) and p38α MAP kinase inhibitory activity in an enzyme assay. The 5-(5-fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles displayed a level of potency similar to that of EW-7197 against both ALK5 (IC50 = 7.68-13.70 nM) and p38α MAP kinase (IC50 = 1240-3370 nM). Among them, I inhibited ALK5 with IC50 value of 7.68 nM in a kinase assay and displayed 82% inhibition at 100 nM in a luciferase reporter assay.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 614750-81-1 belongs to class pyridine-derivatives, name is [1,2,4]Triazolo[1,5-a]pyridine-6-carbaldehyde, and the molecular formula is C7H5N3O, Name: [1,2,4]Triazolo[1,5-a]pyridine-6-carbaldehyde.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Norman, Mark H. published the artcileStructural elucidation of an oxazolo[5,4-b]pyridine: an alternative cyclization product related to nevirapine, Recommanded Product: 2-Chloro-4-methylpyridin-3-amine, the main research area is mol structure oxazolopyridine; nevirapine derivative; pyridooxazole structure; crystal structure oxazolopyridine.

An unexpected cyclization product was isolated in the final step of the synthesis of nevirapine, a non-nucleoside inhibitor of HIV-1 reverse transcriptase. Based on IR spectrometry, mass spectrometry, and a number of two-dimensional NMR experiments, the structure of this product was assigned to be 2-((2-cyclopropylamino)-3-pyridyl)-7-methyloxazolo[5,4-b]pyridine. Results of a single crystal X-ray anal. confirmed this structural assignment. This product arises from cyclization of N-(2-chloro-4-methyl-3-pyridyl)-2-(cyclopropylamine)-3-pyridinecarboxamide, 8, by displacement of the chlorine with the amide carbonyl oxygen. A competitive reaction occurs when 8 is deprotonated prior to cyclization to form nevirapine, 11-cyclopropyl-5,11-dihydro-4-methyl-6H- dipyrido[3,2-b:2′,3′-e][1,4]diazepin-6-one.

Journal of Heterocyclic Chemistry published new progress about Crystal structure. 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, Recommanded Product: 2-Chloro-4-methylpyridin-3-amine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Fang, Zhen published the artcileDiscovery of a potent and selective inhibitor of histone lysine demethylase KDM4D, Quality Control of 197958-29-5, the publication is European Journal of Medicinal Chemistry (2021), 113662, database is CAplus and MEDLINE.

Histone lysine demethylase 4D (KDM4D) plays an important role in the regulation of tumorigenesis, progression and drug resistance and has been considered a potential target for cancer treatment. However, there is still a lack of potent and selective KDM4D inhibitors. In this investigation, we report a new class of KDM4D inhibitors containing the 2-(aryl(pyrrolidine-1-yl)methyl)phenol scaffold, identified through AlphaLisa-based screening, structural optimization, and structure-activity relationship analyses. Among these inhibitors, 24s (I) was the most potent, with an IC₅₀ value of 0.023 ± 0.004μM. This compound exhibited more than 1500-fold selectivity towards KDM4D vs. KDM4A as well as other JMJD subfamily members, indicating good selectivity for KDM4D. Kinetic anal. indicated that 24s did not occupy the 2-oxoglutarate binding pocket. In an in vitro assay, 24s significantly suppressed the proliferation and migration of colorectal cancer (CRC) cells. Overall, this study has identified a good tool compound to explore the biol. function of KDM4D and a good lead compound for drug discovery targeting KDM4D.

European Journal of Medicinal Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Quality Control of 197958-29-5.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Wang, Qingqing published the artcilePreparation of 2-pyridylboronic acid, Computed Properties of 197958-29-5, the publication is Bengbu Yixueyuan Xuebao (2010), 35(10), 1043-1045, database is CAplus.

The means of preparing 2-pyridylboronic acid was investigated. The product was synthesized with 2-bromopyridine, tris-trimethylsilylborate and iPrMgCl as Grignard reagents under N₂, and identified by 1H-NMR. 2-Pyridylboronic acid was synthesized with the yield of 67.7% on conditions of n(tris-trimethylsilylborate): n(2-bromopyridine)=2:1; the reaction temperature was 0 degree, the reaction time 3 h and the hydrolysis temperature 0 degree. 2-Pyridylboronic acid can be synthesized by Grignard reaction on moderate conditions with high yield, which may contribute to the study of pyridine drugs.

Bengbu Yixueyuan Xuebao published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C19H14Cl2, Computed Properties of 197958-29-5.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Lian, Lingxiang published the artcilePhosphine oxide-directed palladium-catalyzed B(3)-H arylation of o-carboranes, Safety of 2-Pyridinylboronic acid, the publication is Tetrahedron Letters (2020), 61(51), 152625, database is CAplus.

The selective functionalization of carboranes has received increasing research interests due to their wild applications in chem., life, and material sciences. Among various structurally diverse carboranes, the development of selective functionalization of the com. available o-carborane (1,2-C₂B₁₀H₁₂) has largely focused on the two acidic C-H bonds. By contrast, research on the activation of the other ten hydridic cage B-H vertexes is relatively less explored. Of particularly challenging, the most electron-deficient nature of B(3,6)-H bonds render very few synthetic methods available for their functionalization. Herein, the authors develop a phosphine oxide-directed Pd-catalyzed highly B(3)-H selective arylation of o-carboranes under very mild reaction conditions in short reaction time.

Tetrahedron Letters published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Safety of 2-Pyridinylboronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Ovchinnikov, V. G. published the artcileCatalytic hydrogenation of 4-nitro-2-methylpyridine N-oxide, Quality Control of 18437-58-6, the publication is Zhurnal Prikladnoi Khimii (Sankt-Peterburg, Russian Federation) (1989), 62(7), 1577-86, database is CAplus.

Catalytic hydrogenation of 4-nitro-2-methylpyridine N-oxide (I) at high pressures and temperatures in low-boiling organic solvents gave 90-98% yields of 4-amino-2-methylpyridine (II). Similar hydrogenations at atm. pressure and room temperature gave mixtures of variously reduced products. Thus, hydrogenation of I over Ni/kieselguhr at 120°, 110 atm, 1 h in Me₂CO gave 98% II.

Zhurnal Prikladnoi Khimii (Sankt-Peterburg, Russian Federation) published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C6H8N2, Quality Control of 18437-58-6.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Chen, Jian Jeffrey published the artcileDevelopment of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer’s disease, Computed Properties of 197958-29-5, the publication is Bioorganic & Medicinal Chemistry Letters (2015), 25(4), 767-774, database is CAplus and MEDLINE.

The β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer’s disease. We used a structure- and property-based drug design approach to identify 2-aminooxazoline 3-azaxanthenes as potent BACE1 inhibitors which significantly reduced CSF and brain Aβ levels in a rat pharmacodynamic model. Compared to the initial lead 2, compound 28 exhibited reduced potential for QTc prolongation in a non-human primate cardiovascular safety model.

Bioorganic & Medicinal Chemistry Letters published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Computed Properties of 197958-29-5.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

An, Peng published the artcileSterically Shielded, Stabilized Nitrile Imine for Rapid Bioorthogonal Protein Labeling in Live Cells, Application of 2-Pyridinylboronic acid, the publication is Journal of the American Chemical Society (2018), 140(14), 4860-4868, database is CAplus and MEDLINE.

In pursuit of fast bioorthogonal reactions, reactive moieties have been increasingly employed for selective labeling of biomols. in living systems, posing a challenge in attaining reactivity without sacrificing selectivity. To address this challenge, here the authors report a bioinspired strategy in which mol. shape controls the selectivity of a transient, highly reactive nitrile imine dipole. By tuning the shape of structural pendants attached to the ortho position of the N-aryl ring of diaryltetrazoles, precursors of nitrile imines, the authors discovered a sterically shielded nitrile imine that favors the 1,3-dipolar cycloaddition over the competing nucleophilic addition The photogenerated nitrile imine exhibits an extraordinarily long half-life of 102 s in aqueous medium, owing to its unique mol. shape that hinders the approach of a nucleophile as shown by DFT calculations The utility of this sterically shielded nitrile imine in rapid (� min) bioorthogonal labeling of glucagon receptor in live mammalian cells was demonstrated.

Journal of the American Chemical Society published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Application of 2-Pyridinylboronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem