Category: 156-83-2

Related Products of 156-83-2, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 156-83-2, Name is 6-Chloropyrimidine-2,4-diamine, SMILES is NC1=CC(Cl)=NC(N)=N1, belongs to pyrimidines compound. In a article, author is Duong Ngoc Toan, introduce new discover of the category.

Quinoline-pyrimidine hybrid compounds from 3-acetyl-4-hydroxy-1-methylquinolin-2(1H)-one: Study on synthesis, cytotoxicity, ADMET and molecular docking

Some novel 2-amino-6-aryl-4-(4′-hydroxy-N-methylquinolin-2′-on-3′-yl)pyrimidines have been synthesized from alpha,beta-unsaturated ketones of 3-acetyl-4-hydroxy-N-methylquinolin-2-one by reaction of corresponding alpha,beta-unsaturated ketones with guanidine hydrochloride. The purity and structure of the obtained products have been confirmed by thin layer chromatography, IR, H-1 NMR, C-13 NMR, HSQC, HMBC and MS spectra. All the synthesized of 3-(2-amino-6-arylpyrimi din-4-yl)-4-hydroxy-1-methylquinolin-2(1H)-ones 6a-i were screened for their in vitro cytotoxic activity against human hepatocellular carcinoma HepG2 and squamous cell carcinoma KB cancer lines. Compounds 6b and 6e had the best activity in the series, with IC50 values equal to 1.33 mu M. Compounds 6a-g exhibited weak or insignificant activity with liver cancer cell lines HepG2, while compounds 6a and 6g had more powerful activity in this sequence, with IC50 values equal to 47.99 and 89.38 mu M, respectively. ADMET properties showed that compounds 6b, 6e, and 6f possessed the drug-likeness behavior. Cross-docking results indicated that two hydrogen bonding interactions in the binding pocket, as potential ligand binding hot-spot residues for compounds 6b and 6e, may be one of the mechanisms of action responsible for the higher cytotoxic effect on HepG2 and KB cells. (C) 2020 The Authors. Published by Elsevier B.V. on behalf of King Saud University.

Related Products of 156-83-2, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 156-83-2 is helpful to your research.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Application of 156-83-2, As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 156-83-2, Name is 6-Chloropyrimidine-2,4-diamine, SMILES is NC1=CC(Cl)=NC(N)=N1, belongs to pyrimidines compound. In a article, author is Kurt, Ibrahim C., introduce new discover of the category.

CRISPR C-to-G base editors for inducing targeted DNA transversions in human cells

CRISPR-guided DNA cytosine and adenine base editors are widely used for many applications(1-4)but primarily create DNA base transitions (that is, pyrimidine-to-pyrimidine or purine-to-purine). Here we describe the engineering of two base editor architectures that can efficiently induce targeted C-to-G base transversions, with reduced levels of unwanted C-to-W (W = A or T) and indel mutations. One of these C-to-G base editors (CGBE1), consists of an RNA-guided Cas9 nickase, anEscherichia coli-derived uracil DNA N-glycosylase (eUNG) and a rat APOBEC1 cytidine deaminase variant (R33A) previously shown to have reduced off-target RNA and DNA editing activities(5,6). We show that CGBE1 can efficiently induce C-to-G edits, particularly in AT-rich sequence contexts in human cells. We also removed the eUNG domain to yield miniCGBE1, which reduced indel frequencies but only modestly decreased editing efficiency. CGBE1 and miniCGBE1 enable C-to-G edits and will serve as a basis for optimizing C-to-G base editors for research and therapeutic applications.

Application of 156-83-2, Consequently, the presence of a catalyst will permit a system to reach equilibrium more quickly, but it has no effect on the position of the equilibrium as reflected in the value of its equilibrium constant.I hope my blog about 156-83-2 is helpful to your research.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 156-83-2, Name is 6-Chloropyrimidine-2,4-diamine, molecular formula is C4H5ClN4. In an article, author is Rolly, Nkulu Kabange,once mentioned of 156-83-2, Recommanded Product: 6-Chloropyrimidine-2,4-diamine.

Drought-induced AtbZIP62 transcription factor regulates drought stress response in Arabidopsis

We investigated the role of AtbZIP62, an uncharacterized Arabidopsis bZIP TF, in oxidative, nitro-oxidative and drought stress conditions using reverse genetics approach. We further monitored the expression of AtPYD1 gene (orthologous to rice OsDHODH1 involved in the pyrimidine biosynthesis) in atbzip62 knock-out (KO) plants in order to investigate the transcriptional interplay of AtbZIP62 and AtPYD1. The atbzip62 KO plants showed significant increase in shoot length under oxidative stress, while no significant difference was recorded for root length compared to WT. However, under nitro-oxidative stress conditions, atbzip62 showed differential response to both NO-donors. Further characterization of AtbZIP62 under drought conditions showed that both atbzip62 and atpyd1-2 showed a sensitive phenotype to drought stress, and could not recover after re-watering. Transcript accumulation of AtbZIP62 and AtPYD1 showed that both were highly up-regulated by drought stress in wild type (WT) plants. Interestingly, AtPYD1 transcriptional level significantly decreased in atbzip62 exposed to drought stress. However, AtbZIP62 expression was highly induced in atpyd1-2 under the same conditions. Both AtbZIP62 and AtPYD1 were up-regulated in atnced3 and atcat2 while showing a contrasting expression pattern in atgsnor13. The recorded increase in CAT, POD, and PPO-like activities, the accumulation of chlorophylls and total carotenoids, and the enhanced proline and malondialdehyde levels would explain the sensitivity level of atbzip62 towards drought stress. All results collectively suggest that AtbZIP62 could be involved in AtPYD1 transcriptional regulation while modulating cellular redox state and photosynthetic processes. In addition, AtbZIP62 is suggested to positively regulate drought stress response in Arabidopsis.

Interested yet? Keep reading other articles of 156-83-2, you can contact me at any time and look forward to more communication. Recommanded Product: 6-Chloropyrimidine-2,4-diamine.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

In an article, author is Sakai, Wataru, once mentioned the application of 156-83-2, COA of Formula: C4H5ClN4, Name is 6-Chloropyrimidine-2,4-diamine, molecular formula is C4H5ClN4, molecular weight is 144.56, MDL number is MFCD00006097, category is pyrimidines. Now introduce a scientific discovery about this category.

Functional impacts of the ubiquitin-proteasome system on DNA damage recognition in global genome nucleotide excision repair

The ubiquitin-proteasome system (UPS) plays crucial roles in regulation of various biological processes, including DNA repair. In mammalian global genome nucleotide excision repair (GG-NER), activation of the DDB2-associated ubiquitin ligase upon UV-induced DNA damage is necessary for efficient recognition of lesions. To date, however, the precise roles of UPS in GG-NER remain incompletely understood. Here, we show that the proteasome subunit PSMD14 and the UPS shuttle factor RAD23B can be recruited to sites with UV-induced photolesions even in the absence of XPC, suggesting that proteolysis occurs at DNA damage sites. Unexpectedly, sustained inhibition of proteasome activity results in aggregation of PSMD14 (presumably with other proteasome components) at the periphery of nucleoli, by which DDB2 is immobilized and sequestered from its lesion recognition functions. Although depletion of PSMD14 alleviates such DDB2 immobilization induced by proteasome inhibitors, recruitment of DDB2 to DNA damage sites is then severely compromised in the absence of PSMD14. Because all of these proteasome dysfunctions selectively impair removal of cyclobutane pyrimidine dimers, but not (6-4) photoproducts, our results indicate that the functional integrity of the proteasome is essential for the DDB2-mediated lesion recognition sub-pathway, but not for GG-NER initiated through direct lesion recognition by XPC.

If you are interested in 156-83-2, you can contact me at any time and look forward to more communication. COA of Formula: C4H5ClN4.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 156-83-2, Name is 6-Chloropyrimidine-2,4-diamine, molecular formula is C4H5ClN4. In an article, author is Piccinni, Viviana,once mentioned of 156-83-2, Application In Synthesis of 6-Chloropyrimidine-2,4-diamine.

Multiscale Conformational Sampling Reveals Excited-State Locality in DNA Self-Repair Mechanism

Ultraviolet (UV) irradiation is known to be responsible for DNA damage. However, experimental studies in DNA oligonucleotides have shown that UV light can also induce sequence-specific self-repair. Following charge transfer from a guanine adenine sequence adjacent to a cyclobutane pyrimidine dimer (CPD), the covalent bond between the two thymines could be cleaved, recovering the intact base sequence. Mechanistic details promoting the self-repair remained unclear, however. In our theoretical study, we investigated whether optical excitation could directly lead to a charge-transfer state, thereby initiating the repair, or whether the initial excited state remains localized on a single nucleobase. We performed conformational sampling of 200 geometries of the damaged DNA double strand solvated in water and used a hybrid quantum and molecular mechanics approach to compute excited states at the complete active space perturbation level of theory. Analysis of the conformational data set clearly revealed that the excited-state properties are uniformly distributed across the fluctuations of the nucleotide in its natural environment. From the electronic wavefunction, we learned that the electronic transitions remained predominantly local on either adenine or guanine, and no direct charge transfer occurred in the experimentally accessed energy range. The investigated base sequence is not only specific to the CPD repair mechanism but ubiquitously occurs in nucleic acids. Our results therefore give a very general insight into the charge locality of UV-excited DNA, a property that is regarded to have determining relevance in the structural consequences following absorption of UV photons.

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Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Synthetic Route of 156-83-2, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 156-83-2, Name is 6-Chloropyrimidine-2,4-diamine, SMILES is NC1=CC(Cl)=NC(N)=N1, belongs to pyrimidines compound. In a article, author is Li, Zhenjiang, introduce new discover of the category.

Application of high-resolution metabolomics to identify biological pathways perturbed by traffic-related air pollution

Background: Substantial research has investigated the adverse effects of traffic-related air pollutants (TRAP) on human health. Convincing associations between TRAP and respiratory and cardiovascular diseases are known, but the underlying biological mechanisms are not well established. High-resolution metabolomics (HRM) is a promising platform for untargeted characterization of molecular mechanisms between TRAP and health indexes. Objectives: We examined metabolic perturbations associated with short-term exposures to TRAP, including carbon monoxide (CO), nitrogen dioxide (NO2), ozone (O-3), fine particulate matter (PM2.5), organic carbon (OC), and elemental carbon (EC) among 180 participants of the Center for Health Discovery and Well-Being (CHDWB), a cohort of Emory University-affiliated employees. Methods: A cross-sectional study was conducted on baseline visits of 180 CHDWB participants enrolled during 2008-2012, in whom HRM profiling was determined in plasma samples using liquid chromatography-high resolution mass spectrometry with positive and negative electrospray ionization (ESI) modes. Ambient pollution concentrations were measured at an ambient monitor near downtown Atlanta. Metabolic perturbations associated with TRAP exposures were assessed following an untargeted metabolome-wide association study (MWAS) framework using feature-specific Tobit regression models, followed by enriched pathway analysis and chemical annotation. Results: Subjects were predominantly white (76.1%) and non-smokers (95.6%), and all had at least a high school education. In total, 7821 and 4123 metabolic features were extracted from the plasma samples by the negative and positive ESI runs, respectively. There are 3421 features significantly associated with at least one air pollutant by negative ion mode, and 1691 features by positive ion mode. Biological pathways enriched by features associated with the pollutants are primarily involved in nucleic acids damage/repair (e.g., pyrimidine metabolism), nutrient metabolism (e.g., fatty acid metabolism), and acute inflammation (e.g., histidine metabolism and tyrosine metabolism). NO2 and EC were associated most consistently with these pathways. We confirmed the chemical identity of 8 metabolic features in negative ESI and 2 features in positive ESI, including metabolites closely linked to oxidative stress and inflammation, such as histamine, tyrosine, tryptophan, and proline. Conclusions: We identified a range of ambient pollutants, including components of TRAP, associated with differences in the metabolic phenotype among the cohort of 180 subjects. We found Tobit models to be a robust approach to handle missing data among the metabolic features. The results were encouraging of further use of HRM and MWAS approaches for characterizing molecular mechanisms underlying exposure to TRAP.

Synthetic Route of 156-83-2, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. I hope my blog about 156-83-2 is helpful to your research.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 156-83-2, Name is 6-Chloropyrimidine-2,4-diamine, SMILES is NC1=CC(Cl)=NC(N)=N1, belongs to pyrimidines compound. In a document, author is Perez-Sanchez, Horacio, introduce the new discover, HPLC of Formula: C4H5ClN4.

Combined Structure and Ligand-Based Design of Selective Acetylcholinesterase Inhibitors

Acetylcholinesterase is a prime target for therapeutic intervention in Alzheimer’s disease. Acetylcholinesterase inhibitors (ACKEIs) are used to improve cognitive abilities, playing therefore an important role in disease management. Drug repurposing screening has been performed on a corporate chemical library containing 11 353 compounds using a target fishing approach comprising three-dimensional (3D) shape similarity and pharmacophore modeling against an approved drug database, Drugbank. This initial screening identified 108 hits. Among them, eight molecules showed structural similarity to the known ACKEI drug, pyridostigmine. Further structure-based screening using a pharmacophore-guided restoring method identifies one more potential hit. Experimental evaluations of the identified hits sieve out a highly selective AChEI scaffold. Further lead optimization using a substructure search approach identifies 24 new potential hits. Three of the 24 compounds (compounds 10b, 10h, and 10i) based on a 6-(2-(pyrrolidin-1-yl)pyrimidin-4-yl)-thiazolo[3,2-alpha]pyrimidine scaffold showed highly promising AChE inhibition ability with IC50 values of 13.10 +/- 0.53, 16.02 +/- 0.46, and 6.22 +/- 0.54 mu M, respectively. Moreover, these compounds are highly selective toward AChE. Compound 10i shows AChE inhibitory activity similar to a known Food and Drug Administration (FDA)-approved drug, galantamine, but with even better selectivity. Interaction analysis reveals that hydrophobic and hydrogen-bonding interactions are the primary driving forces responsible for the observed high affinity of the compound with AChE.

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 156-83-2 is helpful to your research. HPLC of Formula: C4H5ClN4.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Chemistry, like all the natural sciences, Application In Synthesis of 6-Chloropyrimidine-2,4-diamine, begins with the direct observation of nature¡ª in this case, of matter.156-83-2, Name is 6-Chloropyrimidine-2,4-diamine, SMILES is NC1=CC(Cl)=NC(N)=N1, belongs to pyrimidines compound. In a document, author is Fan, Yan, introduce the new discover.

Discovery of 12O-A Novel Oral Multi-Kinase Inhibitor for the Treatment of Solid Tumor

A novel series of pyrimidine-benzotriazole derivatives have been synthesized and evaluated for their anticancer activity against human solid tumor cell lines. The most promising molecule 12O was identified for its excellent antiproliferative activities, especially against the SiHa cell line with IC50 value as 0.009 mu M. Kinase inhibition assay assessed 12O was a potential multi-kinase inhibitor, which possessed potent inhibitory activities against cyclin-dependent kinases (CDKs) and fms-like tyrosine kinase (FLT) with IC50 values in the nanomolar range. Molecular docking studies illustrated that the introduction of triazole moiety in 12O was critical for CDKs inhibition. In addition, 12O inhibited cancer cell proliferation, colony-formation, and cell cycle progression and provoked apoptotic death in vitro. In an SiHa xenograft mouse model, a once-daily dose of compound 12O at 20 mg/kg significantly suppressed the tumor growth without obvious toxicity. Taken together, 12O provided valuable guide for further structural optimization for CDKs and FLT inhibitors.

Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions. you can also check out more blogs about 156-83-2. Application In Synthesis of 6-Chloropyrimidine-2,4-diamine.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

In an article, author is Tigreros, Alexis, once mentioned the application of 156-83-2, Category: pyrimidines, Name is 6-Chloropyrimidine-2,4-diamine, molecular formula is C4H5ClN4, molecular weight is 144.56, MDL number is MFCD00006097, category is pyrimidines. Now introduce a scientific discovery about this category.

Photophysical and crystallographic study of three integrated pyrazolo [1,5-a]pyrimidine-triphenylamine systems

Three new intramolecular charge transfer (ICT) fluorophores having triphenylamine and pyrazolo [1,5-a]pyrimidine moieties 4a-c were synthesized, and their structures were solved by X-ray crystallography (XRC). Compounds 4a, 4b and 4c crystallize in the tetragonal P4(2)/n, triclinic P-1 and monoclinic P2(1)/c space groups with calculated CE-B3LYP structural energies of -104.3, -125.6 and -123.8 kJ/mol, respectively. Substituents effect on molecular and photophysical properties of 4a-c was studied in both solution and solid-state through fluorescence, UV-vis, XRC, and computational methods. The 2-phenyl (4b) and 2-anisyl (2c) derivatives showed better absorption coefficient (4b, epsilon = 76400 -> 119600 M-1 cm(-1) and 4c, epsilon = 66200 -> 89200 M-1 cm(-1)) than 4a (2-Me, epsilon = 9933 -> 21667 M-1 cm(-1)), while the relative quantum yield (phi) in solvents of diverse polarity is as high as phi = 0.98 for 4a, phi = 0.86 for 4b and phi = 0.83 for 4c. For these dyes, Lippert-Mataga correlation were used to estimate the difference between the excited and ground state dipole moments (Delta mu), being 4b the one that suffer the bigger changes with a Delta mu of 26.9 D. Probe 4c is found to be useful as a fluorescent indicators for the qualitative sensing of water content in organic solvents. The solid-state emission data reveal that the antiparallel molecular packing of the crystal structure for 4a-c, with energy framework diagrams influenced mainly by dispersion forces, could disturbs the photophysical properties by changing the donor-acceptor intramolecular coupling. Therefore, the combination of these XRC and photophysical results may constitute in a key input for designing applications in material science.

Interested yet? Read on for other articles about 156-83-2, you can contact me at any time and look forward to more communication. Category: pyrimidines.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia

Let¡¯s face it, organic chemistry can seem difficult to learn. Especially from a beginner¡¯s point of view. Like 156-83-2, Name is 6-Chloropyrimidine-2,4-diamine. In a document, author is Basu, Kallol, introducing its new discovery. Name: 6-Chloropyrimidine-2,4-diamine.

Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264) Part 3: Development of a One-Pot Formylation-Cyclization Sequence to the Diaminopyrimidine Core

The development of a safe, robust, and efficient manufacturing route for the synthesis of diaminopyrimidine 1, a key intermediate to gefapixant citrate (MK-7264), is described. A full mechanistic understanding of the cyclization step in the presence of guanidine was established by performing isotopic labeling experiments and identification of impurities. Guided by the mechanistic understanding, further attempts to modify the cyclization reaction by employing additives to reduce the triazine (9) formation and guanidine loading will also be presented. This newly developed method delivered compound 1 in 88-94% yield on a commercial scale and addressed the shortcomings of the early synthetic route including high PMI, low atom economy, long cycle-time, and multiple purifications to achieve the desired quality.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 156-83-2 help many people in the next few years. Name: 6-Chloropyrimidine-2,4-diamine.

Reference:
Pyrimidine | C4H4N2 – PubChem,
,Pyrimidine – Wikipedia