Month: September 2022

The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. 1722-12-9, formula is C4H3ClN2, Name is 2-Chloropyrimidine. It is also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. COA of Formula: C4H3ClN2.

Gupta, Shiv Shankar;Manisha;Kumar, Rakesh;Dhiman, Ankit Kumar;Sharma, Upendra research published 《 Predictable site-selective functionalization: Promoter group assisted para-halogenation of N-substituted (hetero)aromatics under metal-free condition》, the research content is summarized as follows. Regioselective para-C-H halogenation of N-pyrimidyl (hetero)aromatics (such as 5-bromo-1-(pyrimidin-2-yl)indoline, N-(4-bromophenyl)pyrimidin-2-amine, 6-bromo-1-(pyrimidin-2-yl)-1,2,3,4-tetrahydroquinoline, etc.) through SEAr (electrophilic aromatic substitution) type reaction is disclosed. SEAr type reaction has been utilized for the C5-bromination of indolines (para-selective) (such as 1-(pyrimidin-2-yl)indoline, 6-fluoro-1-pyrimidin-2-yl-2,3-dihydro-1H-indole, 1-pyrimidin-2-yl-2,3-dihydro-1H-indole-2-carboxylic acid Et ester, etc.) with N-bromosuccinimide under metal and additive-free conditions in good to excellent yields. The developed methodol. is also applicable for iodination and challenging chlorination. The pyrimidyl group is identified as a reactivity tuner that also controls the regioselectivity. The present method is also applicable for selective halogenation of aniline, pyridine, indole, oxindole, pyrazole, tetrahydroquinoline, isoquinoline, and carbazole. DFT studies such as Fukui nucleophilicity and natural charge maps also support the observed p-selectivity. Post-functionalization of the title compound into the corresponding arylated, olefinated and dihalogenated products (5-phenyl-1-(pyrimidin-2-yl)indoline, 5-bromo-7-chloro-1-(pyrimidin-2-yl)indoline, (E)-1-(pyrimidin-2-yl)-5-styrylindoline) is achieved in a one-pot, two step fashion. Late-stage C-H bromination was also executed on drug/natural mols. (harmine, etoricoxib, clonidine, and chlorzoxazone) to demonstrate the applicability of the developed protocol.

1722-12-9, 2-Chloropyrimidine is a monochlorinated pyrimidine with plant growth regulating activity. Chloropyrimidine is a useful reagent in the preparation of antivirals and other biologically active compounds.
2-Chloropyrimidine undergoes cobalt-catalyzed cross-coupling reaction with aryl halides.
2-Chloropyrimidine is a molecule that can be synthesized by the oxidation of pyrimidine with hydrogen peroxide and hydrochloric acid. The reaction proceeds through an electrochemical process in which the oxidation catalyst is a platinum electrode. This reaction is catalyzed by the nucleophilic attack of malonic acid on the chloropyrimidine at the methylene group. This efficient method for making 2-chloropyrimidine has been applied to synthesize aryl halides, including phenyl chloropyrimidine and pyridyl chloropyrimidine, from their corresponding chloride and bromide precursors. The fluorescence properties of 2-chloropyrimidine have been studied in coordination chemistry, where it forms complexes with metal ions such as Mn2+. In this study, it was found that adsorption mechanisms are dependent on molecular size, charge density, kinetic energy, and adsorbent surface area., COA of Formula: C4H3ClN2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. One of the three diazines (six-membered heterocyclics with two nitrogen atoms in the ring), it has the nitrogen atoms at positions 1 and 3 in the ring. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Electric Literature of 2927-71-1.

Guo, Weikai;Xing, Yajing;Zhang, Qiansen;Xie, Jiuqing;Huang, Dongxia;Gu, Haijun;He, Peng;Zhou, Miaoran;Xu, Shifen;Pang, Xiufeng;Liu, Mingyao;Yi, Zhengfang;Chen, Yihua research published 《 Synthesis and Biological Evaluation of B-Cell Lymphoma 6 Inhibitors of N-Phenyl-4-pyrimidinamine Derivatives Bearing Potent Activities against Tumor Growth》, the research content is summarized as follows. The transcriptional repressor B-cell lymphoma 6 (BCL6) is frequently misregulated in diffuse large B-cell lymphoma (DLBCL) and has emerged as an attractive drug target for the treatments of lymphoma. In this article, a series of N-phenyl-4-pyrimidinamine derivatives were designed and synthesized as potent BCL6 inhibitors by optimizing hit compound N⁴-(3-chloro-4-methoxyphenyl)-N²-isobutyl-5-fluoro-2,4-pyrimidinediamine on the basis of the structure-activity relationship. Among them, compound I displayed the most potent activities, which significantly blocked the interaction of BCL6 with its corepressors, reactivated BCL6 target genes in a dose-dependent manner, and had better effects compared with the two pos. controls. Further studies indicated that a low dose of I could effectively inhibit germinal center formation. More importantly, I not only showed potent inhibition of DLBCL cell proliferation in vitro but also strongly suppressed the growth of DLBCL in vivo.

2927-71-1, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., Electric Literature of 2927-71-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The systematic study of pyrimidines began in 1884 with Pinner, who synthesized derivatives by condensing ethyl acetoacetate with amidines. Pinner first proposed the name “pyrimidin” in 1885. 109-12-6, formula is C4H5N3, Name is Pyrimidin-2-amine. The parent compound was first prepared by Gabriel and Colman in 1900, by conversion of barbituric acid to 2,4,6-trichloropyrimidine followed by reduction using zinc dust in hot water. Synthetic Route of 109-12-6.

Guo, Ming;Zuo, Daiying;Zhao, Tianming;Li, Xiangyu;Cao, Jianshuang;Qiu, Yuxuan;Wei, Shangfei;Zhai, Xin research published 《 Structure-based optimization identified novel furyl-containing 2,4-diarylaminopyrimidine analogues as ALK/ROS1 dual inhibitors with anti-mutation effects》, the research content is summarized as follows. Aiming to develop ALK/ROS1 dual inhibitors overcoming ceritinib-resistant G1202R mutant, a dedicated structure-guided modification campaign was conducted based on ALK co-crystal structures. Twenty eight diarylaminopyrimidine (DAAP) analogs I [R = methanesulfonyl, acetyl; R¹ = furan-2-yl, oxolan-2-yl, (furan-2-ylmethyl)dimethylamine, etc.; X = O, NH, SO₂] possessing furan or THF group were designed and synthesized, among which compound I [R = methanesulfonyl, R¹ = (furan-2-ylmethyl)dimethylamine, X = S] bearing ((((dimethylamino)methyl)furan-2-yl)methyl)thio fragment was identified. Compound I [R = methanesulfonyl, R¹ = (furan-2-ylmethyl)dimethylamine, X = S] exhibited significant cytotoxicity on ALK-pos. Karpas299 and H2228 cells with IC₅₀ values of 20 nM and 110 nM. Meanwhile, compound I [R = methanesulfonyl, R¹ = (furan-2-ylmethyl)dimethylamine, X = S] turned out as the most potent entity superior to ceritinib with IC₅₀ values of 2.8, 2.6, 3.8 and 2.3 nM against ALKWT, ALKL1196M, ALKG1202R and ROS1WT, resp. Subsequently, western blot assay showed that compound I [R = methanesulfonyl, R¹ = (furan-2-ylmethyl)dimethylamine, X = S] significantly suppressed ALK and its downstream protein expression in a dose-dependent manner. Alternatively, the Hoechst 33258 and AO/EB staining assays illustrated that compound I [R = methanesulfonyl, R¹ = (furan-2-ylmethyl)dimethylamine, X = S] could induce H2228 cell apoptosis. Ultimately, the binding models of compound I [R = methanesulfonyl, R¹ = (furan-2-ylmethyl)dimethylamine, X = S] with ALKWT, ALKG1202R as well as ROS1 clearly presented the essential interactions within the active site. Together, compound I [R = methanesulfonyl, R¹ = (furan-2-ylmethyl)dimethylamine, X = S] was validated as a promising ALK/ROS1 dual inhibitor for ALKG1202R mutation correlated tumors.

109-12-6, 2-Aminopyrimidine is a useful research compound. Its molecular formula is C4H5N3 and its molecular weight is 95.1 g/mol. The purity is usually 95%.
2-Aminopyrimidine is an organic compound that belongs to the group of pyridines. It has been shown to have antimicrobial, antitumor, and antiviral properties. 2-Aminopyrimidine has been used as a fungicide and herbicide in horticulture and agriculture, respectively. The molecular geometry of this molecule is octahedral with coordination geometry C2v. This chemical binds to the BCR-ABL kinase receptor and inhibits its activity by competitive inhibition of ATP binding. 2-Aminopyrimidine has been shown to have a hematologic response in vivo models and in vitro assays. It also has anti-inflammatory effects when it is taken orally or applied topically., Synthetic Route of 109-12-6

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The systematic study of pyrimidines began in 1884 with Pinner, who synthesized derivatives by condensing ethyl acetoacetate with amidines. Pinner first proposed the name “pyrimidin” in 1885. 1722-12-9, formula is C4H3ClN2, Name is 2-Chloropyrimidine. The parent compound was first prepared by Gabriel and Colman in 1900, by conversion of barbituric acid to 2,4,6-trichloropyrimidine followed by reduction using zinc dust in hot water. SDS of cas: 1722-12-9.

Guo, Kang;Gu, Chen;Li, Yun;Xie, Xiaofei;Zhang, Honglin;Chen, Kang;Zhu, Yingguang research published 《 Photoredox Catalyzed Trifluoromethyl Radical-Triggered Trifunctionalization of 5-Hexenenitriles via Cyano Migration》, the research content is summarized as follows. A photoredox catalyzed trifluoromethyl radical-triggered trifunctionalization of 5-hexenenitriles via cyano group migration is reported. The cyano group migration is of high chemo-selectivity even in the presence of aryl or heteroaryl groups as competitors. This protocol provides a facile access to a broad scope of CF₃-containing compounds with high mol. complexity and functional group diversity. The success of gram-scale reaction and the versatility of products in derivative synthesis illustrate the potential value of this transformation in synthetic chem.

SDS of cas: 1722-12-9, 2-Chloropyrimidine is a monochlorinated pyrimidine with plant growth regulating activity. Chloropyrimidine is a useful reagent in the preparation of antivirals and other biologically active compounds.
2-Chloropyrimidine undergoes cobalt-catalyzed cross-coupling reaction with aryl halides.
2-Chloropyrimidine is a molecule that can be synthesized by the oxidation of pyrimidine with hydrogen peroxide and hydrochloric acid. The reaction proceeds through an electrochemical process in which the oxidation catalyst is a platinum electrode. This reaction is catalyzed by the nucleophilic attack of malonic acid on the chloropyrimidine at the methylene group. This efficient method for making 2-chloropyrimidine has been applied to synthesize aryl halides, including phenyl chloropyrimidine and pyridyl chloropyrimidine, from their corresponding chloride and bromide precursors. The fluorescence properties of 2-chloropyrimidine have been studied in coordination chemistry, where it forms complexes with metal ions such as Mn2+. In this study, it was found that adsorption mechanisms are dependent on molecular size, charge density, kinetic energy, and adsorbent surface area., 1722-12-9.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine is a nitrogenous base similar to benzene (a six-membered ring) and includes cytosine, thymine, and uracil as bases used for DNA or RNA. 1722-12-9, formula is C4H3ClN2, Name is 2-Chloropyrimidine. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. COA of Formula: C4H3ClN2.

Guo, Dongdong;Li, Bin;Gao, Wenmei;Zhang, Wuxia;Wang, Yongqiang;Zhao, Jinzhong research published 《 Study on Palladium(II)-Catalyzed Mono-1-alkenylation of 9H-Carbazoles》, the research content is summarized as follows. A general and efficient method is reported for the direct mono-1-alkenylation of 9H-carbazole mols. with divalent palladium as a catalyst and an N-(2-pyridyl)sulfanyl directing group. This method also provides an efficient synthetic route for the synthesis of cross-dialkenylated carbazoles.

COA of Formula: C4H3ClN2, 2-Chloropyrimidine is a monochlorinated pyrimidine with plant growth regulating activity. Chloropyrimidine is a useful reagent in the preparation of antivirals and other biologically active compounds.
2-Chloropyrimidine undergoes cobalt-catalyzed cross-coupling reaction with aryl halides.
2-Chloropyrimidine is a molecule that can be synthesized by the oxidation of pyrimidine with hydrogen peroxide and hydrochloric acid. The reaction proceeds through an electrochemical process in which the oxidation catalyst is a platinum electrode. This reaction is catalyzed by the nucleophilic attack of malonic acid on the chloropyrimidine at the methylene group. This efficient method for making 2-chloropyrimidine has been applied to synthesize aryl halides, including phenyl chloropyrimidine and pyridyl chloropyrimidine, from their corresponding chloride and bromide precursors. The fluorescence properties of 2-chloropyrimidine have been studied in coordination chemistry, where it forms complexes with metal ions such as Mn2+. In this study, it was found that adsorption mechanisms are dependent on molecular size, charge density, kinetic energy, and adsorbent surface area., 1722-12-9.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. 109-12-6, formula is C4H5N3, Name is Pyrimidin-2-amine. In nucleic acids, three types of nucleobases are pyrimidine derivatives: cytosine (C), thymine (T), and uracil (U). Computed Properties of 109-12-6.

Guchhait, Sankar K.;Saini, Meenu;Khivsara, Viren J.;Giri, Santosh K. research published 《 Annulation of Conjugated Azine-Imine with a Sulfoxonium Ylide in a Noncarbenoid Route to Synthesize Multisubstituted Imidazole-Fused Heterocycles》, the research content is summarized as follows. A new [4+1]-annulation of in situ generated heterocyclic azine-aldimines with β-keto sulfoxonium ylides has been developed. The reaction constructs N-fused imidazole rings I (X=Y= CH,N; Ar¹= 4-ClC₆H₄, 4-BrC₆H₄, 4-CNC₆H₄, etc.; Ar² = 4-ClC₆H₄, 4-MeOC₆H₄, 4-FC₆H₄, etc.). In the reaction, the ylides play a dual-functional role of a nucleophilic 1,1-dipolar one-carbon synthon and a source of an internal oxidant, DMSO, that promotes in situ dehydrogenation to product scaffolds. The method enables access to imidazo-pyridine, pyrazine, and pyrimidine heteroaromatics

Computed Properties of 109-12-6, 2-Aminopyrimidine is a useful research compound. Its molecular formula is C4H5N3 and its molecular weight is 95.1 g/mol. The purity is usually 95%.
2-Aminopyrimidine is an organic compound that belongs to the group of pyridines. It has been shown to have antimicrobial, antitumor, and antiviral properties. 2-Aminopyrimidine has been used as a fungicide and herbicide in horticulture and agriculture, respectively. The molecular geometry of this molecule is octahedral with coordination geometry C2v. This chemical binds to the BCR-ABL kinase receptor and inhibits its activity by competitive inhibition of ATP binding. 2-Aminopyrimidine has been shown to have a hematologic response in vivo models and in vitro assays. It also has anti-inflammatory effects when it is taken orally or applied topically., 109-12-6.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine is a nitrogenous base similar to benzene (a six-membered ring) and includes cytosine, thymine, and uracil as bases used for DNA or RNA. 109-12-6, formula is C4H5N3, Name is Pyrimidin-2-amine. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Application In Synthesis of 109-12-6.

Guan, Shengjie;Wu, Fan;Wu, Qian;He, Zhichao;Jiang, Jing;Huang, Yudong;Liu, Li research published 《 Modification of silicone resins by Si-N cross-dehydrocoupling with perfect thermal stability and mechanical performance》, the research content is summarized as follows. A series of new types of modified hydrosilanes were synthesized, using hydrosilanes and nitrogen heterocycles (triethoxysilane, 2-aminopyrimidine, 1,2,4-triazin-3-amine, benzylamine and 2-aminobenzothiazole), by Si-N cross-dehydrocoupling catalyzed by Ru₃CO₁₂. The results of the synthesis were then demonstrated by ¹H NMR and GPC testing. Furthermore, modified silicone resins were obtained by a hydrolytic condensation reaction catalyzed by tetramethylammonium hydroxide and characterized by TGA, DSC and FT-IR. Next, excellent thermal stabilities were determined (best initial decomposition temperature was approx. 400°C, T95% was 595°C, the mass residue rate at 800°C was 87.2%). Carbon fiber reinforced silicone matrix composites were manufactured according to the tech. process developed using DSC and rotary viscometer test results, and the mech. property (ILSS) showed great improvement from 34.8 to 45.8 MPa because of the modification of Si-N cross-dehydrocoupling. After pyrolysis up to 1000°C, the composites still showed a superior ILSS value (19.6 MPa) and the modified silicone resins had a more regular and rounded microstructure and appeared to have ceramic-like particles of Si3N4. This work indicated that the silicone resin (Si-N) modified by cross-dehydrocoupling had greater competitiveness in the field of resin matrix composites.

Application In Synthesis of 109-12-6, 2-Aminopyrimidine is a useful research compound. Its molecular formula is C4H5N3 and its molecular weight is 95.1 g/mol. The purity is usually 95%.
2-Aminopyrimidine is an organic compound that belongs to the group of pyridines. It has been shown to have antimicrobial, antitumor, and antiviral properties. 2-Aminopyrimidine has been used as a fungicide and herbicide in horticulture and agriculture, respectively. The molecular geometry of this molecule is octahedral with coordination geometry C2v. This chemical binds to the BCR-ABL kinase receptor and inhibits its activity by competitive inhibition of ATP binding. 2-Aminopyrimidine has been shown to have a hematologic response in vivo models and in vitro assays. It also has anti-inflammatory effects when it is taken orally or applied topically., 109-12-6.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine is a nitrogenous base similar to benzene (a six-membered ring) and includes cytosine, thymine, and uracil as bases used for DNA or RNA. 554-01-8, formula is C5H7N3O, Name is 4-Amino-5-methylpyrimidin-2(1H)-one. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Quality Control of 554-01-8.

Grytsyk, Natalia;Richert, Ludovic;Didier, Pascal;Dziuba, Dmytro;Ciaco, Stefano;Mazzoleni, Viola;Lequeu, Thiebault;Mori, Mattia;Tor, Yitzhak;Martinez-Fernandez, Lara;Improta, Roberto;Mely, Yves research published 《 Thienoguanosine, a unique non-perturbing reporter for investigating rotational dynamics of DNA duplexes and their complexes with proteins》, the research content is summarized as follows. Time-resolved fluorescence anisotropy (TRFA) provides key information on the dynamics of biomols. and their interaction with ligands. However, since natural nucleosides are almost non-fluorescent, its application to DNA duplexes (dsDNA) requires fluorescent labels, which can alter dsDNA stability, hinder protein binding, and complicate interpretation of TRFA experiments due to their local motion. As shown here, thienoguanosine (thG), a fluorescent analog of guanosine, overcomes all these limitations. We recorded the TRFA decays of thG-labeled dsDNA of different lengths. thG behaved as a rigid, non-perturbing reporter, since no fast correlation time was recorded for any tested dsDNA. Due to its perfect stacking, only two correlation times, instead of the typical three, describe thG-labeled dsDNA rotational dynamics. Thanks to these features, we provided a complete description of the tumbling of the different dsDNA and their complexes with the Set and Ring Associated (SRA) domain of UHRF1, a key epigenetic regulator, obtaining values in excellent agreement with theor. predictions. Moreover, thG was also found sensitive to SRA-induced base flipping of neighboring nucleobases. In the DNA label toolbox, thG thus stands out as a unique reporter for investigating the rotational dynamics of dsDNA and protein/dsDNA complexes.

Quality Control of 554-01-8, 5-Methylcytosine is a methylated form of the nucleobase cytosine occurring predominantly in cytosine-phosphate-guanine (CpG) islands that are produced by DNA methyltransferases and may regulate gene expression. Like cytosine, the DNA sequence containing 5-methylcytosine (5-mC) is able to be replicated without error and 5-mC can pair with guanine in double stranded DNA. However, DNA sequences containing a high local concentration of 5-mC may be less transcriptionally active than areas with higher ratios of unmodified cytosine.
5-Methylcytosine belongs to the class of organic compounds known as hydroxypyrimidines. These are organic compounds containing a hydroxyl group attached to a pyrimidine ring. Pyrimidine is a 6-membered ring consisting of four carbon atoms and two nitrogen centers at the 1- and 3- ring positions. 5-Methylcytosine exists as a solid, slightly soluble (in water), and a very weakly acidic compound (based on its pKa). Within the cell, 5-methylcytosine is primarily located in the cytoplasm. 5-Methylcytosine can be biosynthesized from cytosine. Outside of the human body, 5-methylcytosine can be found in tea. This makes 5-methylcytosine a potential biomarker for the consumption of this food product.
5-methylcytosine is a pyrimidine that is a derivative of cytosine, having a methyl group at the 5-position. It has a role as a human metabolite. It is a member of pyrimidines and a methylcytosine. It derives from a cytosine.
5-Methylcytosine is a nucleic acid that is found in the DNA and RNA of the cell. It is an important component of methylation, which is the process by which a methyl group is added to a molecule. This process can lead to cellular transformation, a process that can cause cancer. 5-Methylcytosine has also been shown as a molecular pathogenesis factor in infectious diseases such as HIV and herpes simplex virus type 1. The presence of 5-methylcytosine in nuclear DNA has been detected by analytical techniques such as gas chromatography/mass spectrometry (GC/MS). There are many analytical methods, including GC/MS, that can be used to detect 5-methylcytosine in cellular nuclei., 554-01-8.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine is a nitrogenous base similar to benzene (a six-membered ring) and includes cytosine, thymine, and uracil as bases used for DNA or RNA. 65-86-1, formula is C5H4N2O4, Name is 2,6-Dioxo-1,2,3,6-tetrahydropyrimidine-4-carboxylic acid. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Formula: C5H4N2O4.

Grosso, Stefano;Marini, Alberto;Gyuraszova, Katarina;Voorde, Johan Vande;Sfakianos, Aristeidis;Garland, Gavin D.;Tenor, Angela Rubio;Mordue, Ryan;Chernova, Tanya;Morone, Nobu;Sereno, Marco;Smith, Claire P.;Officer, Leah;Farahmand, Pooyeh;Rooney, Claire;Sumpton, David;Das, Madhumita;Teodosio, Ana;Ficken, Catherine;Martin, Maria Guerra;Spriggs, Ruth V.;Sun, Xiao-Ming;Bushell, Martin;Sansom, Owen J.;Murphy, Daniel;MacFarlane, Marion;Le Quesne, John P. C.;Willis, Anne E. research published 《 The pathogenesis of mesothelioma is driven by a dysregulated translatome》, the research content is summarized as follows. Malignant mesothelioma (MpM) is an aggressive, invariably fatal tumor that is causally linked with asbestos exposure. The disease primarily results from loss of tumor suppressor gene function and there are no druggable driver oncogenes associated with MpM. To identify opportunities for management of this disease we have carried out polysome profiling to define the MpM translatome. We show that in MpM there is a selective increase in the translation of mRNAs encoding proteins required for ribosome assembly and mitochondrial biogenesis. This in an enhanced rate of mRNA translation, abnormal mitochondrial morphol. and oxygen consumption, and a reprogramming of metabolic outputs. These alterations delimit the cellular capacity for protein biosynthesis, accelerate growth and drive disease progression. Importantly, we show that inhibition of mRNA translation, particularly through combined pharmacol. targeting of mTORC1 and 2, reverses these changes and inhibits malignant cell growth in vitro and in ex-vivo tumor tissue from patients with end-stage disease. Critically, we show that these pharmacol. interventions prolong survival in animal models of asbestos-induced mesothelioma, providing the basis for a targeted, viable therapeutic option for patients with this incurable disease.

Formula: C5H4N2O4, Orotic acid anhydrous is a hydrogen bonding interaction that can be found in biological systems. It plays a role in the physiological effects of orotic acid, which is a metabolite of uridine and an intermediate in the synthesis of pyrimidine nucleotides. Orotic acid has antimicrobial properties and has been shown to inhibit enzyme activities involved in energy metabolism, such as polymerase chain reaction (PCR) and adenosine triphosphate (ATP) synthase. Orotic acid also inhibits the growth of bacteria, fungi, and parasites. Orotic acid anhydrous is used for treating myocardial infarcts or brain functions. The untreated group was given no treatment at all.
Orotic acid, also known as orotate or orotsaeure, belongs to the class of organic compounds known as pyrimidinecarboxylic acids. These are pyrimidines with a structure containing a carboxyl group attached to the pyrimidine ring. Orotic acid exists as a solid, slightly soluble (in water), and a moderately acidic compound (based on its pKa). Orotic acid has been found in human liver and pancreas tissues, and has also been primarily detected in saliva, feces, urine, and blood. Within the cell, orotic acid is primarily located in the cytoplasm and mitochondria. Orotic acid exists in all eukaryotes, ranging from yeast to humans. Orotic acid participates in a number of enzymatic reactions. In particular, Orotic acid can be biosynthesized from L-dihydroorotic acid and quinone; which is mediated by the enzyme dihydroorotate dehydrogenase (quinone), mitochondrial. In addition, Orotic acid and phosphoribosyl pyrophosphate can be converted into orotidylic acid through its interaction with the enzyme uridine monophosphate synthetase isoform a. In humans, orotic acid is involved in the pyrimidine metabolism pathway. Orotic acid is also involved in several metabolic disorders, some of which include the mngie (mitochondrial neurogastrointestinal encephalopathy) pathway, dihydropyrimidinase deficiency, UMP synthase deficiency (orotic aciduria), and Beta ureidopropionase deficiency. Outside of the human body, orotic acid can be found in a number of food items such as green vegetables, alaska blueberry, chickpea, and colorado pinyon. This makes orotic acid a potential biomarker for the consumption of these food products. Orotic acid is a potentially toxic compound. Orotic acid has been found to be associated with several diseases known as phosphoenolpyruvate carboxykinase deficiency 1, cytosolic and hyperornithinemia-hyperammonemia-homocitrullinuria; orotic acid has also been linked to several inborn metabolic disorders including n-acetylglutamate synthetase deficiency, lysinuric protein intolerance, and ornithine transcarbamylase deficiency.
Orotic acid appears as white crystals or crystalline powder.
Orotic acid is a pyrimidinemonocarboxylic acid that is uracil bearing a carboxy substituent at position C-6. It has a role as a metabolite, an Escherichia coli metabolite and a mouse metabolite. It derives from a uracil. It is a conjugate acid of an orotate., 65-86-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. One of the three diazines (six-membered heterocyclics with two nitrogen atoms in the ring), it has the nitrogen atoms at positions 1 and 3 in the ring. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Electric Literature of 2927-71-1.

Griffith, David A.;Edmonds, David J.;Fortin, Jean-Philippe;Kalgutkar, Amit S.;Kuzmiski, J. Brent;Loria, Paula M.;Saxena, Aditi R.;Bagley, Scott W.;Buckeridge, Clare;Curto, John M.;Derksen, David R.;Dias, Joao M.;Griffor, Matthew C.;Han, Seungil;Jackson, V. Margaret;Landis, Margaret S.;Lettiere, Daniel;Limberakis, Chris;Liu, Yuhang;Mathiowetz, Alan M.;Patel, Jayesh C.;Piotrowski, David W.;Price, David A.;Ruggeri, Roger B.;Tess, David A. research published 《 A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor》, the research content is summarized as follows. Peptide agonists of the glucagon-like peptide-1 receptor (GLP-1R) have revolutionized diabetes therapy, but their use has been limited because they require injection. Herein, we describe the discovery of the orally bioavailable, small-mol., GLP-1R agonist PF-06882961 (danuglipron). A sensitized high-throughput screen was used to identify 5-fluoropyrimidine-based GLP-1R agonists that were optimized to promote endogenous GLP-1R signaling with nanomolar potency. Incorporation of a carboxylic acid moiety provided considerable GLP-1R potency gains with improved off-target pharmacol. and reduced metabolic clearance, ultimately resulting in the identification of danuglipron. Danuglipron increased insulin levels in primates but not rodents, which was explained by receptor mutagenesis studies and a cryogenic electron microscope structure that revealed a binding pocket requiring a primate-specific tryptophan 33 residue. Oral administration of danuglipron to healthy humans produced dose-proportional increases in systemic exposure (NCT03309241). This opens an opportunity for oral small-mol. therapies that target the well-validated GLP-1R for metabolic health.

Electric Literature of 2927-71-1, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia