Day: December 1, 2022

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

Vallejo, Luis Felipe published the artcileRenaturation and purification of bone morphogenetic protein-2 produced as inclusion bodies in high-cell-density cultures of recombinant Escherichia coli, COA of Formula: C5H5NO3S, the publication is Journal of Biotechnology (2002), 94(2), 185-194, database is CAplus and MEDLINE.

Escherichia coli was genetically engineered to produce recombinant human bone morphogenetic protein-2 (rhBMP-2) in a non-active aggregated form using a temperature-inducible expression system. High concentrations of both biomass (75 g cell dry weight per L of culture broth) and inactive rhBMP-2 (8.6 g l^-1) were obtained by applying a high-cell-d. cultivation procedure. After washing and solubilizing the inclusion bodies, rhBMP-2 was refolded and dimerized at concentrations up to 100 mg l^-1 by means of a simple dilution method with yields exceeding 50%. Finally, a one-step purification procedure based on affinity chromatog. was implemented to isolate the rhBMP-2 dimer. With the established renaturation and purification protocols, yields of more than 10 mg rhBMP-2 dimer per g cell dry weight were obtained corresponding to 750 mg rhBMP-2 dimer per L of culture broth. The purified rhBMP-2 dimer showed biol. activity equivalent to CHO produced rhBMP-2 as tested by the induction of alk. phosphatase activity in C2C12 cells.

Journal of Biotechnology published new progress about 636-73-7. 636-73-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Sulfonic acid, name is Pyridine-3-sulfonic acid, and the molecular formula is C4H3Cl2N3, COA of Formula: C5H5NO3S.

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

Schneider, Cedric published the artcileDirected ortho-Metalation-Cross-Coupling Strategies. One-Pot Suzuki Reaction to Biaryl and Heterobiaryl Sulfonamides, Application of Pyridine-3-sulfonic acid, the publication is Organic Letters (2011), 13(14), 3588-3591, database is CAplus and MEDLINE.

A general synthesis of stable ortho-boropinacolato aryl and heteroaryl sulfonamides by directed ortho-metalation (DoM) and either MeOBPin or i-PrOBpin electrophile quench is described. A one-pot metalation-Suzuki cross-coupling procedure for the synthesis of biaryls and heterobiaryls, and a complementary DoM-Ir-catalyzed boronation sequence are delineated.

Organic Letters published new progress about 636-73-7. 636-73-7 belongs to pyridine-derivatives, auxiliary class Pyridine,Sulfonic acid, name is Pyridine-3-sulfonic acid, and the molecular formula is C5H5NO3S, Application of Pyridine-3-sulfonic acid.

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

Boot, Arnoud published the artcileAnticancer activity of novel pyrido[2,3-b]indolizine derivatives: the relevance of phenolic substituents, Formula: C7H7ClN2, the publication is Anticancer Research (2014), 34(4), 1673-1678, database is CAplus and MEDLINE.

Background/Aim: The potential of indolizine derivatives as anticancer agents has been shown through recent studies. Herein, we present our exptl. results, showing that pyrido[2,3-b]indolizine derivatives are effective against colorectal cancer (CRC) cell lines. Materials and Methods: Several pyrido[2,3-b]indolizine derivatives were synthesized and their anticancer potential was evaluated against three CRC cell lines and two normal fibroblast cultures. Results: Our experiments identified 4-(3,4)-dihydroxyphenyl)-2-phenylpyrido[2,3-b]indolizine-10-carbonitrile (4f) as being active against all CRC cell lines at concentrations non-cytotoxic against fibroblast cultures. Addnl., cell-cycle anal. indicated that pyrido[2,3-b]indolizines can affect cell-cycle progression, with treated cells accumulating in the S- and G₂/M-phase. Conclusion: The hydroxyl groups in both the 3- and 4- positions of the aromatic substituent on C4 of the indolizine nucleus are crucial for activity against CRC cell lines. Further manipulation of the number and position of hydroxyl substituents on the aromatic rings may lead to improved anticancer activity of this class of compounds

Anticancer Research published new progress about 17281-59-3. 17281-59-3 belongs to pyridine-derivatives, auxiliary class Pyridine,Nitrile,Salt, name is 1-(Cyanomethyl)pyridin-1-ium chloride, and the molecular formula is C7H7ClN2, Formula: C7H7ClN2.

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

Hawlitschek, Christina published the artcileAntihypertensive and cardioprotective effects of different monotherapies and combination therapies in young spontaneously hypertensive rats – A pilot study, Product Details of C17H18N2O6, the publication is Saudi Journal of Biological Sciences (2022), 29(1), 339-345, database is CAplus and MEDLINE.

Spontaneously hypertensive rats (SHR) are an established animal model for antihypertensive treatment. The aim of this pilot study was a systematic search for two lines of antihypertensive treatment – a monotherapy and a combination of two drugs – to be applied in a future study on old SHR. Originally, representatives of three drug classes recommended for antihypertensive therapy in humans should be applied, namely captopril (CAP) as an antagonist of the renin-angiotensin-aldosterone system, nifedipine (NIF) as calcium channel blocker and propranolol (PROP) as β-adrenergic blocker. As we observed that PROP had been poorly ingested, all groups with PROP therapy were excluded from the study. CAP (60 mg kg^-1 d^-1), NIF (10 mg kg^-1 d^-1) or both were administered orally to seven-week-old SHR over 3 wk. A further group of SHR received no treatment (SHR/CTRL). Age-matched normotensive Wistar-Kyoto rats served as normotensive controls. We examined the effect of the antihypertensive therapies on systolic blood pressure, heart weight and on histol. and biochem. markers of cardiac hypertrophy and fibrosis. CAP proved to be the most effective treatment reducing blood pressure and relative heart weight significantly compared to SHR/CTRL without reaching normotensive values. Beginning cardiac fibrosis observed in SHR/CTRL was completely abrogated with CAP treatment. Similar effects were achieved with a combination of CAP and NIF. CAP as monotherapy and CAP + NIF as combination therapy were chosen for the forthcoming study on old SHR.

Saudi Journal of Biological Sciences published new progress about 21829-25-4. 21829-25-4 belongs to pyridine-derivatives, auxiliary class Membrane Transporter/Ion Channel,Calcium Channel, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Product Details of C17H18N2O6.

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

Sturrock, Keith R. published the artcileThe preparation of ketene dithioacetals and thiophenes from chloropyridines containing an active methylene group, COA of Formula: C9H10ClNO2, the publication is Heterocycles (2011), 82(2), 1657-1662, database is CAplus.

The base-catalyzed reaction of CS₂ with the active methylene groups of 6-chloropyridine-3-acetonitrile and -3-acetate, followed by alkylation with reagents also containing active methylene groups, led to ketene dithioacetals. Further reaction with base afforded highly substituted thiophenes.

Heterocycles published new progress about 164464-60-2. 164464-60-2 belongs to pyridine-derivatives, auxiliary class Pyridine,Chloride,Ester, name is Ethyl 2-(2-chloropyridin-3-yl)acetate, and the molecular formula is C9H17NO, COA of Formula: C9H10ClNO2.

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

Ortgies, Stefan published the artcileSelenium-Catalyzed Oxidative C(sp²)-H Amination of Alkenes Exemplified in the Expedient Synthesis of (Aza-)Indoles, Category: pyridine-derivatives, the publication is Organic Letters (2015), 17(11), 2748-2751, database is CAplus and MEDLINE.

A new selenium-catalyzed protocol for the direct, intramol. amination of C(sp²)-H bonds using N-fluorobenzenesulfonimide as the terminal oxidant is reported. This method enables the facile formation of a broad range of diversely functionalized indoles and azaindoles derived from easily accessible ortho-vinyl anilines and vinylated aminopyridines, resp. The procedure exploits the pronounced carbophilicity of selenium electrophiles for the catalytic activation of alkenes and leads to the formation of C(sp²)-N bonds in high yields and with excellent functional group tolerance.

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, Category: pyridine-derivatives.

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

Simler, Thomas published the artcileChromium(II) Pincer Complexes with Dearomatized PNP and PNC Ligands: A Comparative Study of Their Catalytic Ethylene Oligomerization Activity, Category: pyridine-derivatives, the publication is Organometallics (2016), 35(24), 4044-4049, database is CAplus.

Monodeprotonation of the 2,6-bis(di-tert-butylphosphinomethyl)pyridine (^tBuPN^tBuP) at the α-lutidinyl-CH₂ position with 1 equiv of KCH₂C₆H₅ and concomitant dearomatization of the heterocycle afforded K(^tBuP^*N_a^tBuP) (^tBuP^* = di-tert-Bu vinylic P donor, ^tBuP = PtBu₂, N_a = anionic amido N donor); its transmetalation with [CrCl₂(THF)₂] afforded the Cr(II) complex [Cr(^tBuP^*N_a^tBuP)Cl] (A). The x-ray diffraction anal. of A established a slightly distorted square-planar coordination geometry at the metal center and confirmed retention of the dearomatized coordinated ligand. The catalytic activity of A in ethylene oligomerization was studied and compared with that of the related Cr(II) complexes [Cr(^tBuP^*N_aC^NHC)Cl] (B) and [Cr{Cr(^tBuP^*N_a^tBuP^*)Cl}₂] (C) previously reported.

Organometallics published new progress about 338800-13-8. 338800-13-8 belongs to pyridine-derivatives, auxiliary class Bis-phosphine Ligands, name is 2,6-Bis((di-tert-butylphosphino)methyl)pyridine, and the molecular formula is C5H5N3S, Category: pyridine-derivatives.

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

Mallet, Marc published the artcileMigration of lithium in a series of pyridines: double catalysis and reforming. Access to derivatives of 2-bromo-3-lithiopyridine and 4-bromo-2-halo-3-lithiopyridines, Related Products of pyridine-derivatives, the publication is Journal of Organometallic Chemistry (1990), 382(3), 319-32, database is CAplus.

The lithium of an organolithio-pyridinic derivative can be moved from one position to another by an intermol. reaction. Two new reactions are possible for pyridinic organic synthesis; their isomerization of any lithio derivative to a more stable one, and a reaction that transforms a mixture of various bromo-lithio derivatives into a single one. The processes involved and the exptl. tools used are described in terms of the 2-bromo-3-lithio- and 4-bromo-2-halogeno-3-lithiopyridines derivatives synthesis. Thus, 2,6-dibromopyridine was treated with Me₃CLi and (Me₂CH)₂NH in THF followed by DMF to give 40% 2-bromo-3-pyridinecarboxaldehyde.

Journal of Organometallic Chemistry published new progress about 128071-77-2. 128071-77-2 belongs to pyridine-derivatives, auxiliary class Pyridine,Fluoride,Bromide,Aldehyde,Pyridine, name is 4-Bromo-2-fluoronicotinaldehyde, and the molecular formula is C6H3BrFNO, Related Products of pyridine-derivatives.

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

Roth, H. J. published the artcileRing formation and β-elimination by the reaction of triphenylboron on tertiary amines, SDS of cas: 971-66-4, the publication is Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft (1964), 297(12), 766-72, database is CAplus.

Tertiary amino alcs. and tertiary amines of the Mannich-base types were treated with Ph₃B to yield a boron-containing heterocyclic N compound and elimination of an unsaturated moiety. Freshly-prepared, moist Ph₃B (3 g.) in 5 ml. EtOH was added to 2.05 g. 1-phenyl-2-piperidino-l-ethanol in 20 ml. EtOH, and the mixture heated several min. on a steam bath and cooled to give 81% the triphenylboroxazolidine (I), m. 190-1°. N-Methyl-L-ephedrin (1.8 g.), and 1.1 g. 1-phenyl-3-piperidino-1-propanol gave 89% II, m. 207-8°, and 78% III, m. 198-200°, resp. Concentrated EtOH solutions of Et₃N and Ph₃B (stoichiometric equivalents) were allowed to react in the cold and kept a short time to give quant. B,B,B-triphenyl-N,N,N-triethylaminoborane, m. 108-12°. B,B,B-Triphenyl-1-ethylpiperidineborane, m. 114-16°, was similarly prepared from 1-ethylpiperidine. The pyridinyl analog C₅H₅NBPh₃, m. 214-15° (decomposition), was prepared from pyridine and Ph₃B. A solution of 3 g. Ph₃B in 10 ml. absolute EtOH was added to 1.56 g. 2-piperidinomethylcyclohexanone (Mannich base) in 10 ml. EtOH and the solution was evaporated to half its volume on a steam bath and cooled several hrs. to precipitate 85% B,B,B-triphenylpiperidineborane (IV), m. 213-14°. The mother liquor was evaporated in vacuo to a sirup which was dissolved in glacial HOAc and the solution treated with 1 ml. HCl to give 88% the hydrated dimeric cyclohexanone (V), m. 153°. Ph₃B (1.5 g.) in 5 ml. EtOH was added to 5 ml. of an EtOH solution of 2-diethylaminomethylphenol, prepared from 1 g. of the HCl salt by usual procedures. The precipitate, C₄₆H₅₀B₂N₂O, m. 169° (EtOH-acetone). No phenolic, other OH, or NH groups were present, as shown by ir. A similar reaction was carried out with 2-piperidinomethyl-4-methylphenol and Ph₃B. The compound, C₅₀H₅₄B₂N₂O, m. 230° (decomposition), likewise showed no OH or NH groups. IV was obtained by similar reaction of piperidinomethylbenzamide or piperidinomethylsalicylamide with Ph₃B along with BzNH₂, or salicylamide, resp.

Archiv der Pharmazie und Berichte der Deutschen Pharmazeutischen Gesellschaft published new progress about 971-66-4. 971-66-4 belongs to pyridine-derivatives, auxiliary class Pyridine,Benzene, name is Triphenyl(pyridin-1-ium-1-yl)borate, and the molecular formula is C23H20BN, SDS of cas: 971-66-4.

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