Category: 197958-29-5

Dumas, Megan E. published the artcileDual inhibition of Kif15 by oxindole and quinazolinedione chemical probes, Category: pyridine-derivatives, the publication is Bioorganic & Medicinal Chemistry Letters (2019), 29(2), 148-154, database is CAplus and MEDLINE.

The mitotic spindle is a microtubule-based machine that segregates a replicated set of chromosomes during cell division. Many cancer drugs alter or disrupt the microtubules that form the mitotic spindle. Microtubule-dependent mol. motors that function during mitosis are logical alternative mitotic targets for drug development. Eg5 (Kinesin-5) and Kif15 (Kinesin-12), in particular, are an attractive pair of motor proteins, as they work in concert to drive centrosome separation and promote spindle bipolarity. Furthermore, we hypothesize that the clin. failure of Eg5 inhibitors may be (in part) due to compensation by Kif15. In order to test this idea, we screened a small library of kinase inhibitors and identified GW108X, an oxindole that inhibits Kif15 in vitro. We show that GW108X has a distinct mechanism of action compared with a com. available Kif15 inhibitor, Kif15-IN-1 and may serve as a lead with which to further develop Kif15 inhibitors as clin. relevant agents.

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, Category: pyridine-derivatives.

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

Guckian, Kevin published the artcilePyrazolone based TGFβR1 kinase inhibitors, Category: pyridine-derivatives, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(1), 326-329, database is CAplus and MEDLINE.

Interruption of TGFβ signaling through inhibition of the TGFβR1 kinase domain may prove to have beneficial effect in both fibrotic and oncol. diseases. Herein we describe the SAR of a novel series of TGFβR1 kinase inhibitors containing a pyrazolone core. Most TGFβR1 kinase inhibitors described to date contain a core five-membered ring bearing N as H-bond acceptor. Described herein is a novel strategy to replace the core structure with pyrazolone ring, in which the carbonyl group is designed as an H-bond acceptor to interact with catalytic Lys 232.

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, Category: pyridine-derivatives.

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

Dardir, Amira H. published the artcileSynthesis of Triarylmethanes via Palladium-Catalyzed Suzuki-Miyaura Reactions of Diarylmethyl Esters, Category: pyridine-derivatives, the publication is Organometallics (2021), 40(14), 2332-2344, database is CAplus and MEDLINE.

The synthesis of triarylmethanes via Pd-catalyzed Suzuki-Miyaura reactions between diarylmethyl 2,3,4,5,6-pentafluorobenzoates and aryl boronic acids is described. The system operates under mild conditions and has a broad substrate scope, including the coupling of diphenylmethanol derivatives that do not contain extended aromatic substituents. This is significant as these substrates, which result in the types of triarylmethane products that are prevalent in pharmaceuticals, have not previously been compatible with systems for diarylmethyl ester coupling. Also, the reaction can be performed stereospecifically to generate stereoinverted products. From DFT calculations, probably the oxidative addition of the diarylmethyl 2,3,4,5,6-pentafluorobenzoate substrate occurs via an S_N2 pathway, which results in the inverted products. Mechanistic studies indicate that oxidative addition of the diarylmethyl 2,3,4,5,6-pentafluorobenzoate substrates to (IPr)Pd(0) results in the selective cleavage of the O-C(benzyl) bond in part because of a stabilizing η³-interaction between the benzyl ligand and Pd. This is in contrast to previously described Pd-catalyzed Suzuki-Miyaura reactions involving Ph esters, which involve selective cleavage of the C(acyl)-O bond, because there is no stabilizing η³-interaction. It is anticipated that this fundamental knowledge will aid the development of new catalytic systems, which use esters as electrophiles in cross-coupling reactions.

Organometallics 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, Category: pyridine-derivatives.

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

Kuduk, Scott D. published the artcileQuinolizidinone Carboxylic Acids as CNS Penetrant, Selective M₁ Allosteric Muscarinic Receptor Modulators, Safety of 2-Pyridinylboronic acid, the publication is ACS Medicinal Chemistry Letters (2010), 1(6), 263-267, database is CAplus and MEDLINE.

Pos. allosteric modulation of the M₁ muscarinic receptor represents an approach to treat the cognitive decline in patients with Alzheimer’s disease. Replacement of a quinolone ring system in a quinolone carboxylic acid series of M₁ modulators with a quinolizidinone bearing a basic amine linkage led to a series of compounds with higher free fraction, enhanced CNS exposure, and improved efficacy in rodent in vivo models of cognition.

ACS 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, Safety of 2-Pyridinylboronic acid.

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

Bursavich, Matthew G. published the artcileNovel benzofuran-3-one indole inhibitors of PI3 kinase-α and the mammalian target of rapamycin: hit to lead studies, Application of 2-Pyridinylboronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(8), 2586-2590, database is CAplus and MEDLINE.

A series of benzofuran-3-one indole phosphatidylinositol-3-kinases (PI3K) inhibitors identified via HTS has been prepared The optimized inhibitors possess single digit nanomolar activity against p110α (PI3K-α), good pharmaceutical properties, selectivity vs. p110γ (PI3K-γ), and tunable selectivity vs. the mammalian target of rapamycin (mTOR). Modeling of compounds I (R = H; CH₂CH₂CH₂NMe₂) in homol. models of PI3K-α and mTOR supports the proposed rationale for selectivity. Compounds show activity in multiple cellular proliferation assays with signaling through the PI3K pathway confirmed via phospho-Akt inhibition in PC-3 cells.

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, Application of 2-Pyridinylboronic acid.

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

Billingsley, Kelvin L. published the artcileA general and efficient method for the Suzuki-Miyaura coupling of 2-pyridyl nucleophiles, Formula: C5H6BNO2, the publication is Angewandte Chemie, International Edition (2008), 47(25), 4695-4698, database is CAplus and MEDLINE.

One of the most general systems for the cross-coupling of aryl and heteroaryl bromides and chlorides R¹X (R¹ = 4-n-BuC₆H₄, 2,5-Me₂C₆H₃, 3-pyridyl, 5-pyrimidyl, 4-isoquinolinyl, etc.; X = Cl, Br) with 2-pyridyl-derived nucleophiles R²B(OCHMe₂)₃Li [R² = 2-pyridyl, 5-fluoro-2-pyridyl, 6-methoxy-2-pyridyl, 6-(1,3-dioxolan-2-yl)-2-pyridyl] with formation of 2-aryl-substituted pyridines has been developed. The best catalysts were comprised from [Pd₂(dba)₃] and either di-Ph or di(tert-butyl) phosphine oxide.

Angewandte Chemie, International Edition 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, Formula: C5H6BNO2.

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

Calugi, Lorenzo published the artcileSuzuki and Heck Processes for the Synthesis of New Anthraquinone-Based Glycoconjugated Dyes, Safety of 2-Pyridinylboronic acid, the publication is ChemistrySelect (2018), 3(8), 2235-2239, database is CAplus.

Starting from a bromo-anthraquinone dye, different aryl- and styril- derivates are obtained following Suzuki and Heck procedures. Bathochromic shifts are displayed for the products, if compared to the starting anthraquinone dye. Two of these dyes, coming from either the Suzuki and the Heck processes, have been glycosylated with a piperazinyl-lactose derivative, so that two naturalized species are finally obtained. Therefore, the disperse chromophores were transformed in water soluble direct species. These kinds of dyes allow to avoid azo- structures, that are object of growing criticism in the European Union due to their environmental impact.

ChemistrySelect 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

Thomas, Michael published the artcileScaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis, Product Details of C5H6BNO2, the publication is Journal of Medicinal Chemistry (2021), 64(9), 5905-5930, database is CAplus and MEDLINE.

There is an urgent need for new treatments for visceral leishmaniasis (VL), a parasitic infection which impacts heavily large areas of East Africa, Asia, and South America. We previously reported on the discovery of GSK3494245/DDD01305143 (1) as a preclin. candidate for VL and, herein, we report on the medicinal chem. program that led to its identification. A hit from a phenotypic screen was optimized to give a compound with in vivo efficacy, which was hampered by poor solubility and genotoxicity. The work on the original scaffold failed to lead to developable compounds, so an extensive scaffold-hopping exercise involving medicinal chem. design, in silico profiling, and subsequent synthesis was utilized, leading to the preclin. candidate. The compound was shown to act via proteasome inhibition, and we report on the modeling of different scaffolds into a cryo-EM structure and the impact this has on our understanding of the series’ structure-activity relationships.

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 C12H10O4S, Product Details of C5H6BNO2.

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

Martinez, Kristina published the artcilePhotophysics of Ru(II) complexes with hydroxylated diimine ligands: Photoinduced electron/proton transfer to anthraquinone, Name: 2-Pyridinylboronic acid, the publication is Polyhedron (2021), 115376, database is CAplus.

This manuscript reports the reaction of the ³MLCT excited states of two luminescent chromophores, [(bpy)₂Ru(OHbpy)]²⁺ and [(bpy)₂Ru(OMebpy)]²⁺ (bpy = 2,2â€?bipyridine, OHbpy = 4-hydroxy-2,2â€?bipyridine, OMebpy = 4-methoxy-2,2â€?bipyridine), with anthraquinone (AQ). A series of luminescence, electrochem., spectrophotometric and transient absorption studies were done in order to determine free energies for the potential reaction paths between the photoexcited complexes and AQ. For the OMebpy complex, only excited state electron transfer (ET*) from the ³MLCT state of the complex to AQ was possible. However, for the OHbpy complex, the excited state could react with AQ via a variety of pathways including excited state electron transfer, ET*, excited state proton transfer (PT*) and excited state proton coupled electron transfer (PCET*). The thermodn. anal. revealed that, for the OHbpy complex PT* was very endergonic and not a viable reaction pathway, however both ET* and PCET* could occur. Luminescence quenching studies revealed that both the OHbpy and the OMebpy excited complexes reacted with AQ (k_q âˆ?10⁹ M^-1s^-1 for both). Transient absorption anal. showed that, for the OMebpy complex, no photoproducts escaped the encounter complex associated with the quenching reaction. The result is consistent with strong electrostatic association of the 3+/1- encounter complex. For the OHbpy complex transient absorption results clearly show the formation of PCET* products from the encounter complex. The result represents one of a small number of examples of excited states of chromophores reacting via proton coupled electron transfer within an encounter complex.

Polyhedron 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, Name: 2-Pyridinylboronic acid.

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

Kolekar, Yuvraj A. published the artcilePd-Catalyzed Oxidative Aminocarbonylation of Arylboronic Acids with Unreactive Tertiary Amines via C-N Bond Activation, HPLC of Formula: 197958-29-5, the publication is Journal of Organic Chemistry (2021), 86(20), 14028-14035, database is CAplus and MEDLINE.

An efficient synthesis of tertiary amides from aryl boronic acids and inert tertiary amines through the oxidative carbonylation via C(sp³)-N bond activation is presented. This protocol significantly restricts the homocoupling biarylketone product. It involves the use of a homogeneous PdCl₂/CuI catalyst and a heterogeneous Pd/C based catalyst, which promotes C(sp³)-N bond activation of tertiary amines with aryl boronic acids. This process represents a ligand-free, base-free, and recyclable catalyst along with an ideal oxidant like mol. oxygen.

Journal of Organic 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, HPLC of Formula: 197958-29-5.

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