Category: 1722-12-9

Application of 1722-12-9, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 1722-12-9, Name is 2-Chloropyrimidine, SMILES is ClC1=NC=CC=N1, belongs to pyrimidines compound. In a article, author is Zhou, Yujia, introduce new discover of the category.

Functional Dependency Analysis Identifies Potential Druggable Targets in Acute Myeloid Leukemia

Simple Summary New drugs are needed for treating acute myeloid leukemia (AML). We analyzed data from genome-edited leukemia cells to identify druggable targets. These targets were necessary for AML cell survival and had favorable binding sites for drug development. Two lists of genes are provided for target validation, drug discovery, and drug development. The deKO list contains gene-targets with existing compounds in development. The disKO list contains gene-targets without existing compounds yet and represent novel targets for drug discovery. Refractory disease is a major challenge in treating patients with acute myeloid leukemia (AML). Whereas the armamentarium has expanded in the past few years for treating AML, long-term survival outcomes have yet to be proven. To further expand the arsenal for treating AML, we searched for druggable gene targets in AML by analyzing screening data from a lentiviral-based genome-wide pooled CRISPR-Cas9 library and gene knockout (KO) dependency scores in 15 AML cell lines (HEL, MV411, OCIAML2, THP1, NOMO1, EOL1, KASUMI1, NB4, OCIAML3, MOLM13, TF1, U937, F36P, AML193, P31FUJ). Ninety-four gene KOs met the criteria of (A) specifically essential to AML cell survival, (B) non-essential in non-AML cells, and (C) druggable according to three-dimensional (3D) modeling or ligand-based druggability scoring. Forty-four of 94 gene-KOs (47%) had an already-approved drug match and comprised a drug development list termed deKO. Fifty of 94 gene-KOs (53%) had no drug in development and comprised a drug discovery list termed disKO. STRING analysis and gene ontology categorization of the disKO targets preferentially cluster in the metabolic processes of UMP biosynthesis, IMP biosynthesis, dihydrofolate metabolism, pyrimidine nucleobase biosynthesis, vitellogenesis, and regulation of T cell differentiation and hematopoiesis. Results from this study serve as a testable compendium of AML drug targets that, after validation, may be translated into new therapeutics.

Application of 1722-12-9, 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 1722-12-9 is helpful to your research.

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

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. Product Details of 1722-12-9, 1722-12-9, Name is 2-Chloropyrimidine, SMILES is ClC1=NC=CC=N1, in an article , author is Chen, Yang, once mentioned of 1722-12-9.

Uncovering the antitumor effects and mechanisms of Shikonin against colon cancer on comprehensive analysis

Background: Shikonin, a naphthoquinone compound extracted from the root of Lithospermum erythrorhizon, has been extensively studied for its antitumor activity. However, the systematic pathways involved in Shikonin intervention in human colon cancer has not yet clearly defined. Purpose: This study was to evaluate the cytotoxic effects of Shikonin in colon cancer, as well as investigate the potential biomarkers from a global perspective and the possible antitumor mechanisms involved. Methods: In this work, cell viability, cell cycle and cell apoptosis in human colon cancer cells were assessed to evaluate the antitumor activity of Shikonin. Transcriptomics and metabolomics were integrated to provide the perturbed pathways and explore the potential mechanisms. The crucial proteins and genes involved were further validated by immunohistochemistry and real-time quantitative PCR. Results: Shikonin revealed a remarkable antitumor potency in colon cancer. Cell cycle was significantly arrested at the S phase as well as apoptosis was induced in SW480 cell line. Furthermore, a total of 1642 differentially expressed genes and 40 metabolites were detected after Shikonin intervention. The integrated analysis suggested that the antitumor effect was mainly attributed to purine metabolism, arginine biosynthesis, pyrimidine metabolism, urea cycle and metabolism of amino acids. The up-regulated expression of proteins vital for arginine biosynthesis was subsequently validated by immunohistochemistry in xenograft mice. Notably, supplemental dNTPs and arginine could significantly reverse the cytotoxic effect induced by Shikonin and the genes participating in purine metabolism and arginine biosynthesis were further determined by RT-qPCR. Conclusion: Our findings provide a systematic perspective in the therapeutic effect of Shikonin which might lay a foundation for further research on Shikonin in colon cancer.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! 1722-12-9, you can contact me at any time and look forward to more communication. Product Details of 1722-12-9.

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

Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 1722-12-9, Name is 2-Chloropyrimidine, molecular formula is C4H3ClN2, belongs to pyrimidines compound. In a document, author is Xu, Pengtao, introduce the new discover, HPLC of Formula: C4H3ClN2.

Region-specific metabolic characterization of the type 1 diabetic brain in mice with and without cognitive impairment

Type 1 diabetes (T1D) has been reported to cause cognitive decline, but brain metabolic changes during this process are still far from being fully understood. Here, we found that streptozotocin (STZ)-induced T1D mice exhibited impaired learning and memory at 11 weeks after STZ treatment but not at 3 weeks. Therefore, we studied metabolic alterations in six different brain regions of T1D mice with and without cognitive decline, and attempted to identify key metabolic pathways related to diabetic cognitive dysfunction. The results demonstrate that lactate had already increased in all brain regions of T1D mice prior to cognitive decline, but a decreased TCA cycle was only observed in hippocampus, cortex and striatum of T1D mice with cognitive impairment. Reduced N-acetylaspartate and choline were found in all brain regions of T1D mice, irrespective of cognitive decline. In addition, disrupted neurotransmitter metabolism was noted to occur in T1D mice before cognitive deficit. Of note, we found that the level of uridine was significantly reduced in cerebellum, cortex, hypothalamus and midbrain of T1D mice when cognitive decline was presented. Therefore, brain region-specific metabolic alterations may comprise possible biomarkers for the early-diagnosis and monitoring of diabetic cognitive decline. Moreover, down-regulated TCA cycle and pyrimidine metabolism could be closely related to T1D-associated cognitive impairment.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law. In my other articles, you can also check out more blogs about 1722-12-9. HPLC of Formula: C4H3ClN2.

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

Synthetic Route of 1722-12-9, The transformation of simple hydrocarbons into more complex and valuable products via catalytic C¨CH bond functionalisation has revolutionised modern synthetic chemistry. 1722-12-9, Name is 2-Chloropyrimidine, SMILES is ClC1=NC=CC=N1, belongs to pyrimidines compound. In a article, author is Hoarau, Marie, introduce new discover of the category.

Discovery of new non-pyrimidine scaffolds as Plasmodium falciparum DHFR inhibitors by fragment-based screening

In various malaria-endemic regions, the appearance of resistance has precluded the use of pyrimidine-based antifolate drugs. Here, a three-step fragment screening was used to identify new non-pyrimidine Plasmodium falciparum dihydrofolate reductase (PfDHFR) inhibitors. Starting from a 1163-fragment commercial library, a two-step differential scanning fluorimetry screen identified 75 primary fragment hits. Subsequent enzyme inhibition assay identified 11 fragments displaying IC50 in the 28-695 mu M range and selectivity for PfDHFR. In addition to the known pyrimidine, three new anti-PfDHFR chemotypes were identified. Fragments from each chemotype were successfully co-crystallized with PfDHFR, revealing a binding in the active site, in the vicinity of catalytic residues, which was confirmed by molecular docking on all fragment hits. Finally, comparison with similar non-hit fragments provides preliminary input on available growth vectors for future drug development.

Synthetic Route of 1722-12-9, Each elementary reaction can be described in terms of its molecularity, the number of molecules that collide in that step. The slowest step in a reaction mechanism is the rate-determining step.you can also check out more blogs about 1722-12-9.

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

1722-12-9, Name is 2-Chloropyrimidine, molecular formula is C4H3ClN2, belongs to pyrimidines compound, is a common compound. In a patnet, author is Himmelstoss, Maximilian, once mentioned the new application about 1722-12-9, Application In Synthesis of 2-Chloropyrimidine.

2 ‘-O-Trifluoromethylated RNA – a powerful modification for RNA chemistry and NMR spectroscopy

New RNA modifications are needed to advance our toolbox for targeted manipulation of RNA. In particular, the development of high-performance reporter groups facilitating spectroscopic analysis of RNA structure and dynamics, and of RNA-ligand interactions has attracted considerable interest. To this end, fluorine labeling in conjunction with F-19-NMR spectroscopy has emerged as a powerful strategy. Appropriate probes for RNA previously focused on single fluorine atoms attached to the 5-position of pyrimidine nucleobases or at the ribose 2 ‘-position. To increase NMR sensitivity, trifluoromethyl labeling approaches have been developed, with the ribose 2 ‘-SCF3 modification being the most prominent one. A major drawback of the 2 ‘-SCF3 group, however, is its strong impact on RNA base pairing stability. Interestingly, RNA containing the structurally related 2 ‘-OCF3 modification has not yet been reported. Therefore, we set out to overcome the synthetic challenges toward 2 ‘-OCF3 labeled RNA and to investigate the impact of this modification. We present the syntheses of 2 ‘-OCF3 adenosine and cytidine phosphoramidites and their incorporation into oligoribonucleotides by solid-phase synthesis. Importantly, it turns out that the 2 ‘-OCF3 group has only a slight destabilizing effect when located in double helical regions which is consistent with the preferential C3 ‘-endo conformation of the 2 ‘-OCF3 ribose as reflected in the (3)J (H1 ‘-H2 ‘) coupling constants. Furthermore, we demonstrate the exceptionally high sensitivity of the new label in F-19-NMR analysis of RNA structure equilibria and of RNA-small molecule interactions. The study is complemented by a crystal structure at 0.9 angstrom resolution of a 27 nt hairpin RNA containing a single 2 ‘-OCF3 group that well integrates into the minor groove. The new label carries high potential to outcompete currently applied fluorine labels for nucleic acid NMR spectroscopy because of its significantly advanced performance.

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

Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Motloch, Petr, once mentioned the application of 1722-12-9, Name is 2-Chloropyrimidine, molecular formula is C4H3ClN2, molecular weight is 114.53, MDL number is MFCD00006060, category is pyrimidines. Now introduce a scientific discovery about this category, Product Details of 1722-12-9.

Cooperative assembly of H-bonded rosettes inside a porphyrin nanoring

The melamine center dot barbiturate H-bonded rosette motif is of comparable dimensions and symmetry to the cavity of a butadiyne-linked 6-porphyrin nanoring. Functionalisation of each of the barbiturate components and the pyrimidine components of a H-bonded rosette with a pyridine ligand leads to a self-assembled hexapyridine ligand, which binds cooperatively to the zinc porphyrin nanoring. UV-vis-NIR and H-1 NMR experiments show that the 7-component assembly forms at concentrations at which neither the H-bonding interactions nor the zinc porphyrin-pyridine interactions are formed in the absence of one of the three components. The mean effective molarities of these rosette complexes are around 200 mM in chloroform at 298 K.

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

Reference of 1722-12-9, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 1722-12-9, Name is 2-Chloropyrimidine, SMILES is ClC1=NC=CC=N1, belongs to pyrimidines compound. In a article, author is Yang, Feng, introduce new discover of the category.

A novel LC-MS/MS method for quantification of unstable endogenous 3,4-dihydroxyphenylacetaldehyde in rat brain after chemical derivatization

3,4-dihydroxyphenylacetaldehyde (DOPAL), a toxic intermediary metabolite of dopamine (DA), causes catecholaminergic neurodegeneration via covalent binding with functional proteins or other biomolecules. Accurate quantification of DOPAL is essential to investigate the etiological factors associated with DOPAL and the pathogenetic role of DOPAL in Parkinson’s disease (PD). However, no validated quantitative methods are available. Quantification of DOPAL in biosample is challenging since it is a reactive endogenous aldehyde with poor ionization efficiency and chromatographic behavior in the LC-MS system. Here, a sensitive, simple, and robust UPLC-MS/MS method has been established and validated for the determination of DOPAL in rat brain tissue specimens. DOPAL was found to be unstable in biosample due to reactive aldehyde whereas it was stable in acidic condition. The analyte was stabilized by pH and temperature control during the sample preparation and derivatization. Then, a chemical derivatization method that can be readily performed in acidic conditions and at low temperature was employed using 2-hydrazino-4-(trifluoromethyl)-pyrimidine (HTP) to block the reactive aldehyde and improve the detection sensitivity (about 100-fold increase) and chromatographic retention. Bovine serum albumin was used as a surrogate matrix, which was validated by the parallelism assay and post-column infusion experiment. This method was fully validated and the lower limit of quantification (LLOQ) was 0.5 ng/mL. With the method, a significant increase of DOPAL level was found in striatum region of rats received 6-hydroxydopamine (6-OHDA) injection for 12 h, indicating DOPAL may play a pathogenic role in 6-OHDA-induced PD model. (C) 2020 Elsevier B.V. All rights reserved.

Reference of 1722-12-9, Because enzymes can increase reaction rates by enormous factors and tend to be very specific, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 1722-12-9.

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

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature. Formula: C4H3ClN2, 1722-12-9, Name is 2-Chloropyrimidine, SMILES is ClC1=NC=CC=N1, in an article , author is Li, Jia-hui, once mentioned of 1722-12-9.

Synthesis, herbicidal activity study and molecular docking of novel pyrimidine thiourea

According to the pharmacophore binding strategy and principle of bioelectronic isobaric, used the sulfonylurea bridge as the parent structure, a series of novel thiourea compounds containing aromatic-substituted pyrimidines were designed and synthesized. The preliminary herbicidal activity tests showed that some compounds had good herbicidal activity against Digitaria adscendens, Amaranthus retroflexus, especially for compound 4d and 4f. The results showed that compound 4d had an inhibition rate of 81.5% on the root growth of Brassica napus L. at the concentration of 100 mg L-1, and compound 4f had an inhibition rate of 81% on the root growth of Digitaria adscendens at the concentration of 100 mg L-1. Compounds 4d and 4f had higher comparative activity on Echinochloa crus-galli than the commercial herbicide bensulfuron-methyl. The preliminary structure-activity relationship (SAR) was also summarized. We also tested the in vivo AHAS enzyme activity inhibition experiment of 14 compounds at 100 mg L-1, and the results showed that they all have inhibitory activity on the enzyme, with the highest inhibition rate reaching 44.4% (compound 4d). Based on the results of molecular docking to yeast acetohydroxyacid synthase (AHAS), the possible herbicidal activity mechanism of these compounds was evaluated.

But sometimes, even after several years of basic chemistry education, it is not easy to form a clear picture on how they govern reactivity! 1722-12-9, you can contact me at any time and look forward to more communication. Formula: C4H3ClN2.

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

In an article, author is Lin Junjie, once mentioned the application of 1722-12-9, COA of Formula: C4H3ClN2, Name is 2-Chloropyrimidine, molecular formula is C4H3ClN2, molecular weight is 114.53, MDL number is MFCD00006060, category is pyrimidines. Now introduce a scientific discovery about this category.

Efficient Synthesis of Pyridine [2,3-d]pyrimidine Derivatives by Catalyst-free Tandem Cyclization Under Microwave Irradiation

This work presents a highly efficient and simple method for the synthesis of pyridine [2, 3-d] pyrimidine derivatives. This method took the alpha, beta-unsaturated ketones compounds and 1, 3-dimethyl-6-aminouracil as raw material, 28 pyridine [2, 3-d] pyrimidine derivatives were synthesized by microwave irradiation high-efficiency tandem cyclization in 5-15 min without catalyst, including 21 compounds did not see the literature. This method has the characteristics of simple and easy raw materials, high green efficiency, high bonding efficiency and simple post-treatment.

Interested yet? Read on for other articles about 1722-12-9, you can contact me at any time and look forward to more communication. COA of Formula: C4H3ClN2.

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

Reference of 1722-12-9, Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis. The appropriate choice of redox mediator can avoid electrode passivation and overpotential. 1722-12-9, Name is 2-Chloropyrimidine, SMILES is ClC1=NC=CC=N1, belongs to pyrimidines compound. In a article, author is Pragathi, Y. J., introduce new discover of the category.

Design, Synthesis, and Anticancer Activity of 1,3,4-Oxadiazole Incorporated 5-(Pyrimidin-5-yl)benzo[d]oxazole Derivatives

A novel series of 5-(pyrimidin-5-yl)benzo[d]oxazole derivatives has been synthesized, and the chemical structures of products have been determined by H-1 and C-13 NMR, and mass spectra. The products have been tested for their anticancer activity against a panel of human cancer cell lines such as MCF-7 (breast cancer), A549 (lung cancer), Colo-205 (colon cancer), and A2780 (ovarian cancer) using MTT assay. Some tested compounds have demonstrated significant anticancer activity higher than that of the reference drug.

Reference of 1722-12-9, 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 1722-12-9 is helpful to your research.

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