Category: 39856-58-1

Zhang, Yong published the artcileDiscovery of 4-Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents, HPLC of Formula: 39856-58-1, the publication is ACS Medicinal Chemistry Letters (2018), 9(11), 1117-1122, database is CAplus and MEDLINE.

The multi-functional cytokine TGFβ plays a central role in regulating antitumor immunity. It has been postulated that inhibition of TGFβ signaling in concert with checkpoint blockade will provide improved and durable immune response against tumors. Herein, we describe a novel series of 4-azaindole TGFβ receptor kinase inhibitors with excellent selectivity for TGFβ receptor 1 kinase. The combination of compound 3f and an antimouse-PD-1 antibody demonstrated significantly improved antitumor efficacy compared to either treatment alone in a murine tumor model.

ACS Medicinal Chemistry Letters published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C39H35N5O8, HPLC of Formula: 39856-58-1.

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

Liang, Ren-Xiao published the artcileEnantioselective Arylation of Tetrasubstituted Enamines: Access to Enantioenriched Indolenine and 1H-Indole Derivatives, Application of 2-Bromopyridin-3-amine, the publication is ACS Catalysis (2021), 11(3), 1827-1832, database is CAplus.

Palladium-catalyzed intramol. enantioselective β-arylation of tetrasubstituted endocyclic and exocyclic enamines was developed. A range of optically active medium-ring fused indolenines or 3,3′-spiroindolenines were achieved in enantiomeric ratios up to 98:2 with Cs₂CO₃ or K₃PO₄ as the base in the presence of chiral PHOX ligands. The use of Ag₃PO₄ as a base led to enantioenriched 1H-indoles in good enantiomeric ratios (up to 89:11) with (S)-DIFLUORPHOS as a chiral ligand, which proceeded via a possible domino enamine-isomerization/β-arylation sequence.

ACS Catalysis published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C5H5BrN2, Application of 2-Bromopyridin-3-amine.

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

Liu, Lantao published the artcileAsymmetric Synthesis of Planar Chiral Ferrocenes by Enantioselective Intramolecular C-H Arylation of N-(2-Haloaryl)ferrocenecarboxamides, Application of 2-Bromopyridin-3-amine, the publication is Organic Letters (2014), 16(20), 5336-5338, database is CAplus and MEDLINE.

The palladium-catalyzed intramol. C-H arylation reaction of N-(2-bromoaryl)ferrocenecarboxamides furnishes planar chiral ferrocene derivatives TADDOL-derived phosphoramide ligands induce enantioselectivities ranging from 91:9 to 98:2 er.

Organic Letters published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C5H5BrN2, Application of 2-Bromopyridin-3-amine.

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

Wu, Jing-wei published the artcileSynthesis, biological evaluation and 3D-QSAR studies of 1,2,4-triazole-5-substituted carboxylic acid bioisosteres as uric acid transporter 1 (URAT1) inhibitors for the treatment of hyperuricemia associated with gout, Formula: C5H5BrN2, the publication is Bioorganic & Medicinal Chemistry Letters (2019), 29(3), 383-388, database is CAplus and MEDLINE.

Bromonaphthylmethyltriazolyl thioether lesinurad analogs and bioisosteres such as I were prepared as inhibitors of uric acid transporter 1 (URAT1) for potential use in treating hyperuricemia and gout. I inhibited URAT1 with an IC₅₀ value of 32 nM, 225-fold lower than lesinurad. The pharmacophore for the lesinurad analogs was determined using a 3D-QSAR pharmacophore model; the hypothesis was validated by three methods (cost anal., Fisher’s randomization and leave-one-out).

Bioorganic & Medicinal Chemistry Letters published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C12H10FeO4, Formula: C5H5BrN2.

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

Zhu, Heping published the artcileDiscovery of novel 2-aryl-3-sulfonamido-pyridines (HoAns) as microtubule polymerization inhibitors with potent antitumor activities, Related Products of pyridine-derivatives, the publication is European Journal of Medicinal Chemistry (2021), 113117, database is CAplus and MEDLINE.

In this study, a series of novel 2-aryl-3-sulfonamido-pyridines had been designed, synthesized, and evaluated for their antiproliferative activities in vitro and in vivo. Among them, compound I exhibited the most potent activity with IC₅₀ values ranging from 0.170 to 1.193μM in a panel of cancer cell lines. Mechanistic studies indicated that compound I bound to the colchicine site of β-tubulin, resulting in colony formation inhibition, G2/M phase cell cycle arrest, cell apoptosis as well as increased the generation of ROS in both RKO and SW620 cells. In addition, compound I showed potent anti-vascular activity in vitro. Furthermore, compound I also exhibited outstanding antitumor activity in SW620 xenograft tumor models without observable toxic effects, which was more potent than that of ABT-751. In conclusion, these findings suggest that compound I may be a promising microtubule destabilizing agent and deserves for further development in cancer therapy.

European Journal of Medicinal Chemistry published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C9H7F3O3, Related Products of pyridine-derivatives.

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

Fujinaga, Masayuki published the artcileSynthesis and evaluation of 6-[1-(2-[¹⁸F]fluoro-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline for positron emission tomography imaging of the metabotropic glutamate receptor type 1 in brain, Category: pyridine-derivatives, the publication is Bioorganic & Medicinal Chemistry (2011), 19(1), 102-110, database is CAplus and MEDLINE.

The purpose of this study was to synthesize 6-[1-(2-[¹⁸F]fluoro-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline ([¹⁸F]FPTQ, [¹⁸F]7a) and to evaluate its potential as a positron emission tomog. ligand for imaging metabotropic glutamate receptor type 1 (mGluR1) in the rat brain. Compound [¹⁸F]7a was synthesized by [¹⁸F]fluorination of 6-[1-(2-bromo-3-pyridyl)-5-methyl-1H-1,2,3-triazol-4-yl]quinoline (7b) with potassium [¹⁸F]fluoride. At the end of synthesis, 1280-1830 MBq (n = 8) of [¹⁸F]7a was obtained with >98% radiochem. purity and 118-237 GBq/μmol specific activity using 3300-4000 MBq of [¹⁸F]F^–. In vitro autoradiog. showed that [¹⁸F]7a had high specific binding with mGluR1 in the rat brain. Biodistribution study using a dissection method and small-animal PET showed that [¹⁸F]7a had high uptake in the rat brain. The uptake of radioactivity in the cerebellum was reduced by unlabeled 7a and mGluR1-selective ligand JNJ-16259685 (2), indicating that [¹⁸F]7a had in vivo specific binding with mGluR1. Because of a low amount of radiolabeled metabolite present in the brain, [¹⁸F]7a may have a limiting potential for the in vivo imaging of mGluR1 by PET.

Bioorganic & Medicinal Chemistry published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C5H5BrN2, Category: pyridine-derivatives.

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

Yang, Yu-Ming published the artcileSilver-Mediated Trifluoromethoxylation of (Hetero)aryldiazonium Tetrafluoroborates, HPLC of Formula: 39856-58-1, the publication is Organic Letters (2019), 21(19), 8003-8007, database is CAplus and MEDLINE.

Here we report a silver-mediated trifluoromethoxylation of (hetero)aryldiazonium tetrafluoroborates by converting an aromatic amino group into an OCF₃ group. This method, which can be considered to be a trifluoromethoxylation variation of the classic Sandmeyer-type reaction, uses readily available aryl and heteroaromatic amines as starting materials and AgOCF₃ as trifluoromethoxylating reagents. The broad substrate scope and simple, mild reaction condition made this transformation a valuable method in constructing aryl-OCF₃ bonds.

Organic Letters published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C11H21BF4N2O2, HPLC of Formula: 39856-58-1.

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

Ye, Hao published the artcilePalladium-catalyzed Heck cyclization/carbonylation with formates: synthesis of azaindoline-3-acetates and furoazaindolines, Name: 2-Bromopyridin-3-amine, the publication is Chemical Communications (Cambridge, United Kingdom) (2022), 58(48), 6825-6828, database is CAplus and MEDLINE.

Herein a palladium-catalyzed domino cyclization/carbonylation to access ester-functionalized azaindolines, e.g., I applying formates, e.g., phenylformate as a convenient carbonyl source was reported. All four azaindoline isomers were constructed, exhibiting good functional group compatibility. On this basis, modifying the starting tether on the aminopyridine led to furoazaindolines, e.g., II via an intramol. reductive cyclization after the palladium-catalyzed process.

Chemical Communications (Cambridge, United Kingdom) published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C10H16Br3N, Name: 2-Bromopyridin-3-amine.

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

Jin, Hongwei published the artcileCopper-Catalyzed One-Pot Synthesis of Substituted Benzimidazoles, Recommanded Product: 2-Bromopyridin-3-amine, the publication is Advanced Synthesis & Catalysis (2010), 352(2+3), 347-350, database is CAplus.

A copper-catalyzed one-pot synthesis of functionalized benzimidazoles has been developed. The procedure combines the copper-catalyzed three-component cascade reaction of sulfonyl azides R¹SO₂N₃ (R¹ = Ph, 4-MeC₆H₄, etc.), alkynes R²CCH (R² = Ph, 4-MeC₆H₄, etc.) and 2-X-4-R³-aniline (R³ = H, Me, Cl; X = Br, I) and the copper-catalyzed intramol. N-arylation of sulfonamides in one sequence, which afforded the products I in moderate to good yields.

Advanced Synthesis & Catalysis published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C5H5BrN2, Recommanded Product: 2-Bromopyridin-3-amine.

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

Zhang, Yong published the artcileDiscovery of 4-Azaindole Inhibitors of TGFβRI as Immuno-oncology Agents, HPLC of Formula: 39856-58-1, the publication is ACS Medicinal Chemistry Letters (2018), 9(11), 1117-1122, database is CAplus and MEDLINE.

The multi-functional cytokine TGFβ plays a central role in regulating antitumor immunity. It has been postulated that inhibition of TGFβ signaling in concert with checkpoint blockade will provide improved and durable immune response against tumors. Herein, we describe a novel series of 4-azaindole TGFβ receptor kinase inhibitors with excellent selectivity for TGFβ receptor 1 kinase. The combination of compound 3f and an antimouse-PD-1 antibody demonstrated significantly improved antitumor efficacy compared to either treatment alone in a murine tumor model.

ACS Medicinal Chemistry Letters published new progress about 39856-58-1. 39856-58-1 belongs to pyridine-derivatives, auxiliary class Pyridine,Bromide,Amine, name is 2-Bromopyridin-3-amine, and the molecular formula is C39H35N5O8, HPLC of Formula: 39856-58-1.

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