Category: 150728-13-5

150728-13-5, Name is 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine, molecular formula is C15H10Cl2N4O2, belongs to pyrimidines compound, is a common compound. In a patnet, author is Emami, Leila, once mentioned the new application about 150728-13-5, Application In Synthesis of 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine.

Design, synthesis, molecular simulation, and biological activities of novel quinazolinone-pyrimidine hybrid derivatives as dipeptidyl peptidase-4 inhibitors and anticancer agents

Two novel series of quinazolinone-pyrimidine (series a: 9a-9i) and benzyl-pyrimidine hybrids (series b: 12a-12c) were designed, synthesized and characterized by spectroscopic methods. The dipeptidyl peptidase-4 inhibition potencies of these compounds were assessed through a MAK 203 kit. Compound 9e was found to be the most potent agent with an IC50 value of 34.3 +/- 3.3 mu M. A kinetic study revealed that it acted as a competitive inhibitor. Molecular modeling of these compounds was in agreement with the in vitro results. Due to the crucial role of dipeptidyl peptidase-4 in cancer therapy, the cytotoxic activities of the compounds were also evaluated against three cancerous cell lines (HT-29, SW1116 and A549). Almost all the compounds displayed better antiproliferative activity on colon cancer cell lines (HT-29 and SW1116) compared to a lung cancer cell line (A549). Compounds 9e and 12c exhibited significant activity toward the HT-29 cell line with an IC50 of 10.67 +/- 0.3 mu M and 27.9 +/- 6.5 mu M in comparison to sitagliptin and cisplatin as a positive control, respectively. Among the different cells, the compounds showed the best inhibitory effects on HT-29, which was compatible with the greater expression of the dipeptidyl peptidase-4 marker detected by flow cytometry in this cell line. Further studies on the hit compounds (9e and 12c) through cell cycle and apoptosis assays also showed that these compounds could induce cell death by apoptosis or arrest cells in the G2/M phase. Accordingly, the results imply that 9e is a potent inhibitor of dipeptidyl peptidase-4 with efficient anti-cancer activity and could play a role as a cytotoxic agent in colorectal cancer.

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

Chemistry can be defined as the study of matter and the changes it undergoes. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology. 150728-13-5, Name is 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine, molecular formula is , belongs to pyrimidines compound. In a document, author is Basu, Kallol, Recommanded Product: 150728-13-5.

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.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 150728-13-5, in my other articles. Recommanded Product: 150728-13-5.

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

Catalysts are substances that increase the reaction rate of a chemical reaction without being consumed in the process. 150728-13-5, Name is 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine, SMILES is ClC1=NC(=NC(=C1OC2=C(C=CC=C2)OC)Cl)C3=NC=CC=N3, belongs to pyrimidines compound. In a document, author is Hill, Brian, introduce the new discover, Application In Synthesis of 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine.

A pilot clinical trial of oral tetrahydrouridine/decitabine for noncytotoxic epigenetic therapy of chemoresistant lymphoid malignancies

One mechanism by which lymphoid malignancies resist standard apoptosis-intending (cytotoxic) treatments is genetic attenuation of the p53/p16-CDKN2A apoptosis axis. Depletion of the epigenetic protein DNA methyltransferase 1 (DNMT1) using the deoxycytidine analog decitabine is a validated approach to cytoreduce malignancy independent of p53/p16. In vivo decitabine activity, however, is restricted by rapid catabolism by cytidine deaminase (CDA). We, therefore, combined decitabine with the CDA-inhibitor tetrahydrouridine and conducted a pilot clinical trial in patients with relapsed lymphoid malignancies: the doses of tetrahydrouridine/decitabine used (similar to 10/0.2 mg/kg orally (PO) 2x/week) were selected for the molecular pharmacodynamic objective of non-cytotoxic, S-phase dependent, DNMT1-depletion, guided by previous Phase 1 studies. Patients with relapsed/refractory B- or T-cell malignancies (n = 7) were treated for up to 18 weeks. Neutropenia without concurrent thrombocytopenia is an expected toxicity of DNMT1-depletion and occurred in all patients (Grade 3/4). Subjective and objective clinical improvements occurred in 4 of 7 patients, but these responses were lost upon treatment interruptions and reductions to manage neutropenia. We thus performed parallel experiments in a preclinical in vivo model of lymphoma to identify regimen refinements that might sustain DNMT1-targeting in malignant cells but limit neutropenia. We found that timed-alternation of decitabine with the related molecule 5-azacytidine, and combination with inhibitors of CDA and de novo pyrimidine synthesis could leverage feedback responses of pyrimidine metabolism to substantially increase lymphoma cytoreduction but with less neutropenia. In sum, regimen innovations beyond incorporation of a CDA-inhibitor are needed to sustain decitabine DNMT1-targeting and efficacy against chemo-resistant lymphoid malignancy. Such potential solutions were explored in preclinical in vivo studies. (C) 2020 Elsevier Inc. All rights reserved.

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 150728-13-5 is helpful to your research. Application In Synthesis of 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine.

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

Synthetic Route of 150728-13-5, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 150728-13-5, Name is 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine, SMILES is ClC1=NC(=NC(=C1OC2=C(C=CC=C2)OC)Cl)C3=NC=CC=N3, belongs to pyrimidines compound. In a article, author is El-Badawy, Azza A., introduce new discover of the category.

Acryloyl isothiocyanate skeleton as a precursor for synthesis of some novel pyrimidine, triazole, triazepine, thiadiazolopyrimidine and acylthiourea derivatives as antioxidant agents

The reactions of 2-cyano-3-pyrazolylpropenoyl isothiocyanate derivative 2 with some mono- and bidentate nucleophiles namely, dodecan-1-amine, 6-aminothiouracil, hydrazine, phenylhydrazine, phenylurea, semicarbazide, and thiosemicarbazide, in addition to some derivatives of hydrazides, have been investigated to obtain some valuable heterocyclic skeletons gathering with a pyrazole core, viz. pyrimidine, triazole, triazepine, thiadiazolopyrimidine as well as acylthiourea derivatives. Hydrazinolysis of 2 was found to provide a mixture of thiosemicarbazide, diheterylazine, and triazepine derivatives. Treatment of 2 with phenylhydrazine was mainly dependent on the reaction conditions to produce a mixture of pyrimidinethione and triazole derivatives at room temperature or the triazepine derivative at heating conditions. The antioxidant activity screening of these compounds disclosed that pyrimidinethione derivatives 9 and 13 exhibited the most potency.

Synthetic Route of 150728-13-5, 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 150728-13-5.

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

Synthetic Route of 150728-13-5, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 150728-13-5, Name is 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine, SMILES is ClC1=NC(=NC(=C1OC2=C(C=CC=C2)OC)Cl)C3=NC=CC=N3, belongs to pyrimidines compound. In a article, author is Gong, Yi-Lin, introduce new discover of the category.

Synthesis, Crystal Structure and Biological Activity of 7-(4-Methylpiperazin-1-Yl)-5-[4-(Trifluoromethyl)Phenyl]pyrazolo[1,5-a]Pyrimidine-3-Carbonitrile

The title compound C19H17F3N6 was synthesized and structurally characterized by infrared and mass spectroscopy, H-1 NMR, elemental analyses and single crystal X-ray diffraction. The compound crystallizes in monoclinic system, space group P2(1)/c with a = 17.097(4) angstrom, b = 7.1668(16) angstrom, c = 18.389(3) angstrom, beta = 118.251(15)degrees, V = 1984.8(8) angstrom(3), Z = 4, D-c = 1.293 g cm(-3), F(000) = 800, mu(MoK alpha) = 0.10 mm(-1), R-1 = 0.0667, and wR(2) = 0.2084 for reflections with I > 2 sigma(I). Pyrazolo[1,5-a]pyrimidine and phenyl ring are almost coplanar, and the piperazine ring is in a chair conformation. The crystal structure is stabilized by C-H…N hydrogen interactions and a number of weak pi…pi interactions. In addition, the results of the determination of biological activity showed that the compound exhibited significant inhibitory activity against K562 and MKN45 cancer cell lines.

Synthetic Route of 150728-13-5, The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 150728-13-5 is helpful to your research.

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

Application of 150728-13-5, 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. 150728-13-5, Name is 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine, SMILES is ClC1=NC(=NC(=C1OC2=C(C=CC=C2)OC)Cl)C3=NC=CC=N3, 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.

Application of 150728-13-5, 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 150728-13-5 is helpful to your research.

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

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time. 150728-13-5, Name is 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine, formurla is C15H10Cl2N4O2. In a document, author is Yakout, El-Sayed M. A., introducing its new discovery. HPLC of Formula: C15H10Cl2N4O2.

Bioactive Small Molecules Having a Fatty Residue. Part VI: Synthesis, Cytotoxicity Evaluation, and Molecular Docking Studies of New Pyrimidine Derivatives as Antitumor Agents

Difficultly accessible pyrimidine, thiazolopyrimidine, triazolopyrimidine, and thiazinopyrimidine derivatives containing an oleyl residue were synthesized via alkylation of 6-oleyl-2-thiouracil. The structure of the synthesized compounds was established on the basis of their spectral data, elemental analyses, and chemical behavior. The in vitro cytotoxicity of selected compounds was screened against two human cancer cell lines, MCF-7 breast cancer and HepG2 liver cancer cell lines. 8-[(8Z)-Heptadec-8-en-1-yl)-3-hydroxy-3,4-dihydropyrimido[2,1-b][1,3]thiazin-6(2H)-one turned out to be the most potent with IC50 values of 12.5 and 20 mu g/mL against MCF-7 and HepG2 cancer cell lines, respectively. The structure-activity relationship for this compound was interpreted in terms of molecular docking and molecular dynamics studies.

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 150728-13-5 help many people in the next few years. HPLC of Formula: C15H10Cl2N4O2.

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

Application of 150728-13-5, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 150728-13-5, Name is 4,6-Dichloro-5-(2-methoxyphenoxy)-2,2′-bipyrimidine, SMILES is ClC1=NC(=NC(=C1OC2=C(C=CC=C2)OC)Cl)C3=NC=CC=N3, belongs to pyrimidines compound. In a article, author is Algohary, Ayman M., introduce new discover of the category.

Design, Synthesis And Evaluation Of New Chemosensors Containing Quinazolinones Moiety For Ions In An Aqueous Medium And Biological Samples

Quinazolinone derivatives were reported as a varied range of biological activity and played a principal part metabolism of all biological systems. The quinazolinone is an organic compound ring containing two merged aromatic rings benzene and pyrimidine. The current project deals with the design and synthesizing new Quinazolinones derivatives and evaluate them as colorimetric chemosensors to detect the cations in the aqueous medium and biological sample. The synthetic strategy depends on acylation of anthranilic acid (1) with butyroyl chloride followed by ring closure to yield benzoxazinone (2), which was reacted with various nucleophiles hydrazine hydrate, urea, thiourea, p-aminophenol, hydroxylamine, and phenyl hydrazine to give corresponding quinazolinone chemosensors 3-amino-2-propylquinazolin-4(3H)-ones (4), 6-nitro-4-oxo-2-propylquinazoline-3(4H)-carboxamide (5a), 6-nitro-4-oxo-2-propylquinazoline-3(4H)-carbothioamide (5b), 3-(2-hydroxyphenyl)-6-nitro-2-propylquinazolin-4(3H)-one (6), 3-hydroxy-2-propylquinazolin-4(3H)-ones (7) and 6-nitro-3-(phenylamino)-2-propylquinazolin-4(3H)-one (8). The importance of producing chemosensors has increased in the last decade. Therefore, here we developed and synthesized chemosensors 4 and 8 with high-selectivity and specificity to detect copper and mercury in both aqueous solutions and blood samples. Where the results showed that chemosesors 4 and 8 exhibited colormetric responses from pale yellow to green in case of Cu2+ ions and exhibited remarkable color change from pale yellow to rose by interacting with Hg2+. Chemosensors 5b and 7 show high selectivity toward cadmium ion, whereas chemosensors 5b and 7 exhibited remarkable color change from colorless to yellow when adding Cd2+. but the synthesized compounds 5a and 6 did not exhibit colorimetric response in all cation’s samples. In addition, the synthesized chemosensor was established as a strip paper to make the measurement process easy and inexpensive. All the synthesized compounds have been established by instrumental spectroscopy; 1HNMR, 13CNMR, IR, and mass spectra (ms).

Application of 150728-13-5, 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 150728-13-5 is helpful to your research.

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