Month: November 2022

Olson, Calla M. published the artcileDevelopment of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype, Quality Control of 1702809-17-3, the publication is Cell Chemical Biology (2019), 26(6), 792-803.e10, database is CAplus and MEDLINE.

Cyclin-dependent kinase 7 (CDK7) regulates both cell cycle and transcription, but its precise role remains elusive. We previously described THZ1, a CDK7 inhibitor, which dramatically inhibits superenhancer-associated gene expression. However, potent CDK12/13 off-target activity obscured CDK7s contribution to this phenotype. Here, we describe the discovery of a highly selective covalent CDK7 inhibitor. YKL-5-124 causes arrest at the G1/S transition and inhibition of E2F-driven gene expression; these effects are rescued by a CDK7 mutant unable to covalently engage YKL-5-124, demonstrating on-target specificity. Unlike THZ1, treatment with YKL-5-124 resulted in no change to RNA polymerase II C-terminal domain phosphorylation; however, inhibition could be reconstituted by combining YKL-5-124 and THZ531, a selective CDK12/13 inhibitor, revealing potential redundancies in CDK control of gene transcription. These findings highlight the importance of CDK7/12/13 polypharmacol. for anti-cancer activity of THZ1 and posit that selective inhibition of CDK7 may be useful for treatment of cancers marked by E2F misregulation.

Cell Chemical Biology published new progress about 1702809-17-3. 1702809-17-3 belongs to piperidines, auxiliary class Cell Cycle,CDK, name is (R,E)-N-(4-(3-((5-Chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)piperidine-1-carbonyl)phenyl)-4-(dimethylamino)but-2-enamide, and the molecular formula is C30H32ClN7O2, Quality Control of 1702809-17-3.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Fang, Li published the artcileA Metal-Free Oxidative Cross-Dehydrogenative Coupling of N-Aryl Tetrahydroisoquinolines and 2-Methylazaarenes Using a Recyclable Oxoammonium Salt as Oxidant in Aqueous Media, Related Products of piperidines, the publication is European Journal of Organic Chemistry (2016), 2016(21), 3559-3567, database is CAplus.

A metal-free oxidative cross-dehydrogenative coupling of N-aryl tetrahydroisoquinolines and 2-methylazaarenes in water under mild conditions was developed. 4-Acetylamino-2,2,6,6-tetramethylpiperidine-1-oxoammonium tetrafluoroborate was employed as a mild oxidant that can be recovered and reused directly. The reaction proceeds through formation of an iminium ion in situ followed by condensation with various nucleophiles, providing the desired products in moderate to good yields.

European Journal of Organic Chemistry published new progress about 219543-09-6. 219543-09-6 belongs to piperidines, auxiliary class Piperidine,Fluoride,Salt,Amine,Amide, name is 4-Acetamido-2,2,6,6-tetramethyl-1-oxopiperidinium Tetrafluoroborate, and the molecular formula is C11H21BF4N2O2, Related Products of piperidines.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Liu, Li published the artcileActivation of peroxymonosulfate with CuCo₂O₄@kaolin for efficient degradation of phenacetin, Name: 2,2,6,6-Tetramethylpiperidin-4-one, the publication is Chemical Engineering Journal (Amsterdam, Netherlands) (2020), 126014, database is CAplus.

CuCo₂O₄@kaolin was successfully synthesized by a sol-gel method and used as a heterogeneous catalyst to activate peroxymonosulfate (PMS) for the degradation of phenacetin (PNT). The results demonstrated that 10 mg/L PNT was completely decomposed by 1 mM PMS activated with 0.1 g/L CuCo₂O₄@kaolin within 15 min at initial pH 7. CuCo₂O₄@kaolin exhibited the best excellent catalytic performance among the tested catalysts, and the pseudo-first-order rate constants of PNT degradation were CuCo₂O₄@kaolin (0.40 min^-1) > CuCo₂O₄ (0.22 min^-1) > Co₃O₄@kaolin (0.10 min^-1) > CuO@kaolin (0.08 min^-1) > kaolin (0.02 min^-1). CuCo₂O₄@kaolin also possessed superior stability, and the degradation efficiency of PNT declined from 100% in the first round to 80% in the fourth round. Nevertheless, a simple calcinating treatment (20 min) after the third round could restore its catalytic activity substantially and 95% removal of PNT was realized, 15% higher compared to without treatment. ^·OH, SO₄^·-, and ¹O₂ were the reactive oxygen species driving the PNT degradation Based on the results mentioned above, characterizations of CuCo₂O₄@kaolin, and intermediates of PNT degradation, the possible pathways and underlying mechanisms of the PNT degradation in the CuCo₂O₄@kaolin/PMS system were deduced. CuCo₂O₄@kaolin/PMS had a universal degradation potential toward various organic pollutants, and the degradation efficiencies of sulfisoxazole, p-nitrophenol, chloramphenicol, and 2,4,6-Trichlorophenol reached 95-100% within 5-45 min. Thus, this work provides a novel and efficient PMS activator through an eco-friendly synthetic route, and it may be put into practice to degrade organic matter in wastewater.

Chemical Engineering Journal (Amsterdam, Netherlands) published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C9H17NO, Name: 2,2,6,6-Tetramethylpiperidin-4-one.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Chen, Feng published the artcileHydrogenation of Pyridines Using a Nitrogen-Modified Titania-Supported Cobalt Catalyst, Category: piperidines, the publication is Angewandte Chemie, International Edition (2018), 57(44), 14488-14492, database is CAplus and MEDLINE.

Heterogeneous recyclable catalysts were prepared by pyrolysis of Co(OAc)₂, melamine, and titanium dioxide; in their presence, pyridines underwent chemoselective hydrogenation to piperidines in water under acid-free conditions. The resulting materials show an unusual nitrogen-modified titanium structure through partial incorporation of nitrogen into the support. The catalyst was also used for the preparation of N-isopropylpiperidines by hydrogenation of pyridines in isopropanol.

Angewandte Chemie, International Edition published new progress about 39546-32-2. 39546-32-2 belongs to piperidines, auxiliary class Piperidine,Amine,Amide, name is Piperidine-4-carboxamide, and the molecular formula is C6H12N2O, Category: piperidines.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Liu, Shikai published the artcileAn all-in-one theranostic nanoplatform based on upconversion dendritic mesoporous silica nanocomposites for synergistic chemodynamic/photodynamic/gas therapy, Formula: C9H17NO, the publication is Nanoscale (2020), 12(47), 24146-24161, database is CAplus and MEDLINE.

Gasotransmitters with high therapeutic efficacy and biosafety have been drawing the attention of researchers. Nevertheless, how to effectively deliver gases to and precisely control their generation at the lesion as well as integrate them with other therapies to realize precision therapy have remained elusive. Herein, we report a versatile Cu2+-initiated nitric oxide (NO) nanocomposite for multimodal imaging-guided synergistic chemodynamic/photodynamic/gas therapy. After the nanomedicine was ingested by tumor cells, the acidic tumor microenvironment accelerated the decompn of CuO2 and simultaneously triggered the Fenton-like catalytic reaction of Cu2+ and H2O2 to produce highly toxic OH. By virtue of the NO generation and glutathione depletion, UMNOCC-PEG can relieve the antioxidant capacity and hypoxia of the tumor to improve the efficiency of chemodynamic therapy (CDT) and photodynamic therapy (PDT). Importantly, NO and reactive oxygen species (ROS) can generate reactive nitrogen species (RNS), which can result in DNA damage, further improving the therapeutic effect (cell apoptosis rate up to 93.4%). Moreover, the inherent properties of lanthanide ions endow UMNOCC-PEG with upconversion luminescence (UCL), CT and MRI trimodal imaging capability, achieving precise cancer treatment. By taking advantage of these features, the strategy developed here may provide a promising application foreground to conquer malignant tumors.

Nanoscale published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C9H17NO, Formula: C9H17NO.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Crich, David published the artcileDirect Chemical Synthesis of the β-Mannans: Linear and Block Syntheses of the Alternating β-(1â†?)-β-(1â†?)-Mannan Common to Rhodotorula glutinis, Rhodotorula mucilaginosa, and Leptospira biflexa, Computed Properties of 4972-31-0, the publication is Journal of the American Chemical Society (2004), 126(46), 15081-15086, database is CAplus and MEDLINE.

Two stereocontrolled syntheses of a Me glycoside of an alternating β-(1â†?)-β-(1â†?)-mannohexaose, representative of the mannan from Rhodotorula glutinis, Rhodotorula mucilaginosa, and Leptospira biflexa, are described. Both syntheses employ a combination of 4,6-O-benzylidene- and 4,6-O-p-methoxybenzylidene acetal-protected donors to achieve stereocontrolled formation of the β-mannoside linkage. The first synthesis is a linear one and proceeds with a high degree of stereocontrol throughout and an overall yield of 1.9%. The second synthesis, a block synthesis, makes use of the coupling of two trisaccharides, resulting in a shorter sequence and an overall yield of 4.4%, despite the poor selectivity in the key step.

Journal of the American Chemical Society published new progress about 4972-31-0. 4972-31-0 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-(Phenylsulfinyl)piperidine, and the molecular formula is C11H15NOS, Computed Properties of 4972-31-0.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Chen, Qiumeng published the artcileSize-controllable Fe-N/C single-atom nanozyme with exceptional oxidase-like activity for sensitive detection of alkaline phosphatase, Recommanded Product: 2,2,6,6-Tetramethylpiperidin-4-one, the publication is Sensors and Actuators, B: Chemical (2020), 127511, database is CAplus.

Nanozymes become currently a frontier of chem. research. However, exploiting a novel nanozyme with high activity, good stability and reproducibility is challenging. Here, size-controllable Fe-N/C nanozymes containing exclusive single Fe atoms coordinated Fe-N_x sites were succesfully prepared through a facile pyrolysis of size controllable Fe-Zn ZIFs precursors. The Fe-N/C nanozymes exhibit exceptional high oxidase-mimicking activity able to catalyze oxidation of colorless 3,3′,5,5′-tetramethylbenzidine (TMB) by dissolved oxygen to generate blue product. Their catalytic activities can be regulated by modulating the molar ratios of methanol to metal salts (e.g., Fe and Zn) through which the size controllable Fe-Zn ZIFs precursors are obtained. Upon introduction of ascorbic acid (AA) into Fe-N/C/TMB system, complete inhibition of TMB oxidation was observed, resulting in significant decline in absorbance with a clear color change. In the presence of alk. phosphatase (ALP), ascorbic acid 2-phosphate (AAP) is hydrolyzed to produce AA. When coupled with AAP, a novel colorimetric biosensor platform was fabricated for ALP activity screening in the range of 0.05 U/L-100 U/L (four orders of magnitude) with an ultra-low limit of detection of 0.02 U/L. The work provides a promising strategy to rationally design the transition metal-N/C single-atom nanozyme with high oxidase-like activity.

Sensors and Actuators, B: Chemical published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C9H17NO, Recommanded Product: 2,2,6,6-Tetramethylpiperidin-4-one.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Li, Ning published the artcileCorrelation of active sites to generated reactive species and degradation routes of organics in peroxymonosulfate activation by Co-loaded carbon, Related Products of piperidines, the publication is Environmental Science & Technology (2021), 55(23), 16163-16174, database is CAplus and MEDLINE.

Peroxymonosulfate (PMS)-based advanced oxidation processes (PMS-AOPs) as an efficient strategy for organic degradation are highly dependent on catalyst design and structured active sites. However, the identification of the active sites and their relationship with reaction mechanisms for organic degradation are not fully understood for a composite catalyst due to the complex structure. Herein, we developed a family of Co encapsulated in N-doped carbons (Co-PCN) with tailored types and contents of active sites via manipulated pyrolysis for PMS activation and ciprofloxacin (CIP) degradation, focusing on the correlation of active sites to generated reactive species and degradation routes of organics The structure-function relationships between the different active sites in Co-PCN catalysts and reactive oxygen species (ROS), as well as bond breaking position of CIP, were revealed through regression anal. and d. functional theory calculation Co-N_x, O-C=O, C=O, graphitic N, and defects in Co-PCN stimulate the generation of ¹O₂ for oxidizing the C-C bond in the piperazine ring of CIP into C=O. The substitution of F by OH and hydroxylation of the piperazine ring might be induced by SO₄^â€? and ^{â€?/sup>OH, whose formation was affected by C-O, Co(0), Co-N_x, graphitic N, and defects. The findings provided new insights into reaction mechanisms in PMS-AOP systems and rational design of catalysts for ROS-oriented degradation of pollutants.}

Environmental Science & Technology published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C9H17NO, Related Products of piperidines.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Hu, Erfeng published the artcilePyrolysis behaviors of anaerobic digestion residues in a fixed-bed reactor with rapid infrared heating, HPLC of Formula: 826-36-8, the publication is Environmental Science and Pollution Research (2022), 29(34), 51815-51826, database is CAplus and MEDLINE.

Fast pyrolysis via rapid IR heating may significantly enhance the heat transfer and suppress the secondary reaction of the volatiles. The effects of various pyrolysis temperatures on pyrolysis behaviors of anaerobic digestion residues (ADR) were studied in this research utilizing a fixed-bed reactor equipped with rapid IR heating (IH), as well as to compare the pyrolysis products produced by rapid IR heating (IH) to those produced by conventional elec. heating (EH). Thermogravimetric anal. revealed that pyrolysis of ADR occurred in three decomposition stages. The results of pyrolysis experiments showed that increasing temperature first raised the bio-oil yield for IH and EH, peaking at 500-600°C, but thereafter decreased the yield. In contrast to the findings achieved with EH, IR heating (IH) presented a greater overall bio-oil yield but a lower gas yield. The bio-oil produced by IH increased from 8.35 weight% at 400°C to 12.56 weight% at 500°C before dropping to 11.22 weight% at 700°C. Gaseous products produced by IH have a higher heating value than those generated by EH. Nitrogenous compounds, ketones, and phenols make up the majority of the bio-oil. In the IH bio-oil, nitrogen compounds rose with increasing temperature, while those varied slightly in the EH bio-oil. The phenols content in IH bio-oil was much more than that of EH, exhibiting values of 8.63% and 2.95%, resp. The findings of the FTIR spectra of biochar indicated that as the temperature increased, the chains of aliphatic side professedly reduced and the structure of biochar became considerably ordered for both heating techniques. The Raman spectra of IH biochar showed that the ratio of AG/AD rose progressively from 0.17 to 0.20 as pyrolysis temperature rose from 500 to 700°C.

Environmental Science and Pollution Research published new progress about 826-36-8. 826-36-8 belongs to piperidines, auxiliary class Natural product, name is 2,2,6,6-Tetramethylpiperidin-4-one, and the molecular formula is C9H17NO, HPLC of Formula: 826-36-8.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem

Crich, David published the artcileThe 4-(tert-Butyldiphenylsiloxy)-3-fluorobenzyl Group: A New Alcohol Protecting Group, Fully Orthogonal with the p-Methoxybenzyl Group and Removable under Desilylation Conditions, Safety of 1-(Phenylsulfinyl)piperidine, the publication is Journal of Organic Chemistry (2009), 74(6), 2486-2493, database is CAplus and MEDLINE.

A new benzyl ether-type protecting group for alcs., the 4-(tert-butyldiphenylsiloxy)-3-fluorobenzyl group, is introduced. The protecting group is introduced by means of the readily prepared benzyl bromide and is cleaved with tetrabutylammonium fluoride in DMF under microwave irradiation The fluoride substituent provides stability to oxidizing conditions, such that the new protecting group is fully compatible with the removal of p-methoxybenzyl ethers with DDQ. Applications of the new protecting group in the direct stereocontrolled synthesis of β-mannopyranosides are presented.

Journal of Organic Chemistry published new progress about 4972-31-0. 4972-31-0 belongs to piperidines, auxiliary class Piperidine,Benzene, name is 1-(Phenylsulfinyl)piperidine, and the molecular formula is C11H15NOS, Safety of 1-(Phenylsulfinyl)piperidine.

Referemce:
https://en.wikipedia.org/wiki/Piperidine,
Piperidine | C5H11N – PubChem