Month: October 2022

《2-Aminophenylpyrimidines as Novel Inhibitors of Aminoacyl-tRNA Synthetase Interacting Multifunctional Protein 2 (AIMP2)-DX2 for Lung Cancer Treatment》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Lee, Seungbeom; Kim, Dae Gyu; Kim, Kyeojin; Kim, Taewoo; Lim, Semi; Kong, Hyejin; Kim, Sunghoon; Suh, Young-Ger. SDS of cas: 3934-20-1 The article mentions the following:

Aminoacyl-tRNA synthetase interacting multifunctional proteins (AIMPs) have recently been considered novel therapeutic targets in several cancers. In this publication we report the development of novel 2-aminophenylpyrimidines as new AIMP2-DX2 inhibitors. In particular, aminophenylpyrimidine 3 not only exhibited promising in vitro and in vivo potency but also exerted selective inhibition of H460 and A549 cells and AIMP2-DX2 rather than WI-26 cells and AIMP2. Aminophenylpyrimidine 3 offers possible therapeutic potential in the treatment of lung cancer. In the experimental materials used by the author, we found 2,4-Dichloropyrimidine(cas: 3934-20-1SDS of cas: 3934-20-1)

2,4-Dichloropyrimidine(cas: 3934-20-1) is a member of organic chlorides. Almost all organochlorine compounds are synthesized. It is widely used as intermediates, solvents and pesticides of chemical synthetic products.SDS of cas: 3934-20-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Parmar, Udaysinh; Somvanshi, Dipesh; Kori, Santosh; Desai, Aman A.; Dandela, Rambabu; Maity, Dilip K.; Kapdi, Anant R. published an article in 2021. The article was titled 《Room-Temperature Amination of Chloroheteroarenes in Water by a Recyclable Copper(II)-Phosphaadamantanium Sulfonate System》, and you may find the article in Journal of Organic Chemistry.Electric Literature of C4H2Cl2N2 The information in the text is summarized as follows:

The current report discusses about an efficient copper-based catalytic system (Cu/PTABS) for the amination of chloroheteroarenes RCl (R = pyrazinyl, 1,3-benzothiazol-2-yl, 9H-purin-6-yl, etc.) at ambient temperature in water as the sole reaction solvent, a combination that is first to be reported. A wide variety of chloroheteroarenes could be coupled efficiently with primary and secondary amines, e.g., morpholine as well as selected amino acid esters, e.g., L-valine Me ester hydrochloride under mild reaction conditions. Catalytic efficiency of the developed protocol also promotes late-stage functionalization of active pharmaceutical ingredients, e.g., I (APIs) such as antibiotics (floxacins) and anticancer drugs. The catalytic system also performs efficiently at a very low concentration of 0.0001 mol% (TON = 980,000) and can be recycled 12 times without any appreciable loss in activity. Theor. calculations reveal that the π-acceptor ability of the ligand PTABS is the main reason for the appreciably high reactivity of the catalytic system. Preliminary characterization of the catalytic species in the reaction was carried out using UV-VIS and ESR spectroscopy, providing evidence for the Cu(II) oxidation state. In the experiment, the researchers used many compounds, for example, 2,4-Dichloropyrimidine(cas: 3934-20-1Electric Literature of C4H2Cl2N2)

2,4-Dichloropyrimidine(cas: 3934-20-1) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Electric Literature of C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Zhang, Chufeng; Qi, Wenyan; Li, Yong; Tang, Minghai; Yang, Tao; Liu, Kongjun; Chen, Yong; Deng, Dexin; Xiang, Mingli; Chen, Lijuan published an article in 2021. The article was titled 《Discovery of 3-(4-(2-((1H-Indol-5-yl)amino)-5-fluoropyrimidin-4-yl)-1H-pyrazol-1-yl)propanenitrile Derivatives as Selective TYK2 Inhibitors for the Treatment of Inflammatory Bowel Disease》, and you may find the article in Journal of Medicinal Chemistry.Recommanded Product: 1193-21-1 The information in the text is summarized as follows:

The design, synthesis, and structure-activity relationships (SARs) of 3-(4-(2-((1H-indol-5-yl)amino)-5-fluoropyrimidin-4-yl)-1H-pyrazol-1-yl)propanenitrile I [R5= 2-cyanoethyl; R6 = Me, fluoro; R7 = indolin-5-yl, 1-oxoisoindolin-5-yl, 1-tert-butoxycarbonylindol-5-yl, etc.] as selective TYK2 inhibitors was reported. Among them, compound I [R5 = 2-cyanoethyl; R6 = fluoro; R7 = 1-tert-butoxycarbonylindol-5-yl] exhibited acceptable TYK2 inhibition with an IC50 value of 9 nM, showed satisfactory selectivity characteristics over the other three homologous JAK kinases, and performed good functional potency in the JAK/STAT signaling pathway on lymphocyte lines and human whole blood. In liver microsomal assay studied that the clearance rate and half-life of I [R5 = 2-cyanoethyl; R6 = fluoro; R7 = 1-tert-butoxycarbonylindol-5-yl] were 11.4 mL/min/g and 121.6 min, resp. Furthermore, in a dextran sulfate sodium colitis model, I [R5 = 2-cyanoethyl; R6 = fluoro; R7 = 1-tert-butoxycarbonylindol-5-yl] reduced the production of pro-inflammatory cytokines IL-6 and TNF-α and improved the inflammation symptoms of mucosal infiltration, thickening, and edema. Compound I [R5 = 2-cyanoethyl; R6 = fluoro; R7 = 1-tert-butoxycarbonylindol-5-yl] was aselective TYK2 inhibitor and was used to treat immune diseases and deserved further investigation. In the part of experimental materials, we found many familiar compounds, such as 4,6-Dichloropyrimidine(cas: 1193-21-1Recommanded Product: 1193-21-1)

4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Recommanded Product: 1193-21-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Raubo, Piotr; Carbajo, Rodrigo J.; McCoull, William; Raubo, Joanna; Thomas, Morgan published an article in 2021. The article was titled 《Diversity-orientated synthesis of macrocyclic heterocycles using a double SNAr approach》, and you may find the article in Organic & Biomolecular Chemistry.Recommanded Product: 3934-20-1 The information in the text is summarized as follows:

An efficient macrocyclization approach based on the double aromatic nucleophilic substitution (SNACK) was developed. This methodol. allows a facile incorporation of heterocyclic motifs into macrocyclic rings and rapid synthesis of a significant number of structurally diverse macrocycles e.g., I. SNACK macrocyclization enables preparation of stable diastereoisomers of conformationally restricted macrocycles (atropisomers) e.g., II and e.g., III. Practical application of SNACK macrocyclization in a drug discovery project was exemplified by the identification of high affinity macrocyclic binders of B-cell lymphoma 6 (BCL6). The experimental part of the paper was very detailed, including the reaction process of 2,4-Dichloropyrimidine(cas: 3934-20-1Recommanded Product: 3934-20-1)

2,4-Dichloropyrimidine(cas: 3934-20-1) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Recommanded Product: 3934-20-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pola, Suresh; Shah, Shailesh R.; Pingali, Harikishore; Zaware, Pandurang; Thube, Baban; Makadia, Pankaj; Patel, Hoshang; Bandyopadhyay, Debdutta; Rath, Akshyaya; Giri, Suresh; Patel, Jitendra H.; Ranvir, R. K.; Sundar, S. R.; Patel, Harilal; Kumar, Jeevan; Jain, Mukul R. published an article in 2021. The article was titled 《Discovery of a potent G-protein-coupled receptor 119 agonist for the treatment of type 2 diabetes》, and you may find the article in Bioorganic & Medicinal Chemistry.COA of Formula: C4H2Cl2N2 The information in the text is summarized as follows:

Benzylidenethiazolidinedione as a novel polar head for discovering a new series of GPR119 agonists I [R = H, Me; R1 = methoxycarbonyl, ethoxycarbonyl, tert-butoxycarbonyl, isobutoxycarbonyl, benzyloxycarbonyl] was discussed. The identification of a potent and oral GPR 119 agonist II [R = Me; R1 = tert-butoxycarbonyl], which showed in-vitro potency in the cell-based assay and in-vivo efficacy without exerting any significant signs of toxicity in relevant animal models. In the experimental materials used by the author, we found 4,6-Dichloropyrimidine(cas: 1193-21-1COA of Formula: C4H2Cl2N2)

4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.COA of Formula: C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 1193-21-1In 2020 ,《Selectable and releasable noncovalent functionalization of semiconducting SWCNTs by biethynyl-2,5-bis(dodecoxy)benzene unit-containing conjugated copolymers》 appeared in Macromolecular Chemistry and Physics. The author of the article were Wei, Xia; Maimaitiyiming, Xieraili. The article conveys some information:

A rigid structural unit diethynyl-2,5-bis(dodecoxy)benzene (DDB) is proposed to functionalize single-walled carbon nanotubes (SWCNTs) with the assistance of pyrimidine ring. The effectiveness of conjugated polymer extraction of semiconducting SWCNTs is demonstrated by absorption and Raman spectroscopy. The protonated pyrimidine ring by the trifluoroacetic acid is used to reduce the interaction between polymer and SWCNTs that the bound wrapping polymer can be removed from the sorted SWCNTs, and mol. dynamics simulations of the binding ability of DDB and pyrimidine units to SWCNTs are conducted to further illustrate the strong binding ability of DDB units to SWCNTs. Therefore, this work provides an effective structural and theor. reference for polymer separation or modification of semiconducting SWCNTs. The experimental part of the paper was very detailed, including the reaction process of 4,6-Dichloropyrimidine(cas: 1193-21-1Related Products of 1193-21-1)

4,6-Dichloropyrimidine(cas: 1193-21-1) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Related Products of 1193-21-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

SDS of cas: 90213-66-4In 2010 ,《Synthesis and SAR of Novel 4-Morpholinopyrrolopyrimidine Derivatives as Potent Phosphatidylinositol 3-Kinase Inhibitors》 appeared in Journal of Medicinal Chemistry. The author of the article were Chen, Zecheng; Venkatesan, Aranapakam M.; Dehnhardt, Christoph M.; Ayral-Kaloustian, Semiramis; Brooijmans, Natasja; Mallon, Robert; Feldberg, Larry; Hollander, Irwin; Lucas, Judy; Yu, Ker; Kong, Fangming; Mansour, Tarek S.. The article conveys some information:

A series of (4-morpholino)pyrrolopyrimidine derivatives were synthesized and evaluated as inhibitors of PI3Kα and mTOR, leading to the discovery of PI3Kα selective inhibitors (e.g., I) and dual PI3Kα/mTOR kinase inhibitors (e.g., II). PI3Kα/mTOR dual inhibitors demonstrated inhibition of tumor cell growth in vitro and in vivo and caused suppression of the pathway specific biomarkers [e.g., the phosphorylation of Akt at Thr308 (T308) and Ser473 (S473)] in the human breast cancer cell line MDA361. In addition, compound II demonstrated good in vivo efficacy in the MDA361 human breast tumor xenograft model. In the part of experimental materials, we found many familiar compounds, such as 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4SDS of cas: 90213-66-4)

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. 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. SDS of cas: 90213-66-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application In Synthesis of 5-Bromo-4,6-dihydroxypyrimidineOn November 1, 1989 ,《Inhibition of uridine phosphorylase from Giardia lamblia by pyrimidine analogs》 appeared in Biochemical Pharmacology. The author of the article were Jimenez, Barbara M.; Kranz, Peter; Lee, Choy Soong; Gero, Annette M.; O’Sullivan, William J.. The article conveys some information:

Fifty-six pyrimidine analogs were tested as possible inhibitors of uridine phosphorylase from G. lamblia. Values of Ki were determined for eight of these which demonstrated an inhibition >60% under the standard conditions of uridine at 1 mM (approx. 1.5 times the Km) and inhibitor at 1 mM. All were competitive with respect to uridine. The most effective inhibitors were uracil analogs substituted at the C-5 position with electron-withdrawing groups (nitro groups or halogens). The inhibitory effect at the 5-position appeared to be further enhanced by substitution at the C-6 position with electron-releasing groups. The order of effectiveness as inhibitors was 6-methyl-5-nitrouracil > 6-amino-5-nitrouracil > 5-benzylacyclouridine > 5-nitrouracil > 5-fluorouracil > 5-bromouracil > 6-benzyl-2-thiouracil > 1,3-dimethyluracil, with Ki values of 10, 12, 44, 56, 119, 230, 190 and >1000 μM, resp. The compounds were also effective inhibitors of the thymidine phosphorylase activity of the enzyme. The results are discussed in relation to the use of these pyrimidine analogs to treat G. lamblia infections. The experimental part of the paper was very detailed, including the reaction process of 5-Bromo-4,6-dihydroxypyrimidine(cas: 15726-38-2Application In Synthesis of 5-Bromo-4,6-dihydroxypyrimidine)

5-Bromo-4,6-dihydroxypyrimidine(cas: 15726-38-2) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Application In Synthesis of 5-Bromo-4,6-dihydroxypyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Safety of 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amineOn November 30, 2011 ,《Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity》 appeared in Nature Biotechnology. The author of the article were Anastassiadis, Theonie; Deacon, Sean W.; Devarajan, Karthik; Ma, Haiching; Peterson, Jeffrey R.. The article conveys some information:

Small-mol. protein kinase inhibitors are widely used to elucidate cellular signaling pathways and are promising therapeutic agents. Owing to evolutionary conservation of the ATP-binding site, most kinase inhibitors that target this site promiscuously inhibit multiple kinases. Interpretation of experiments that use these compounds is confounded by a lack of data on the comprehensive kinase selectivity of most inhibitors. Here we used functional assays to profile the activity of 178 com. available kinase inhibitors against a panel of 300 recombinant protein kinases. Quant. anal. revealed complex and often unexpected interactions between protein kinases and kinase inhibitors, with a wide spectrum of promiscuity. Many off-target interactions occur with seemingly unrelated kinases, revealing how large-scale profiling can identify multitargeted inhibitors of specific, diverse kinases. The results have implications for drug development and provide a resource for selecting compounds to elucidate kinase function and for interpreting the results of experiments involving kinase inhibitors. In addition to this study using 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine, there are many other studies that have used 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8Safety of 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine) was used in this study.

7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics. Safety of 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 1972,Canadian Journal of Chemistry included an article by Neville, G. A.; Avdovich, H. W.. Name: 6-Methoxypyrimidine-2,4(1H,3H)-dione. The article was titled 《Isomeric pyrimidone and uracil derivatives obtained by reaction of barbiturates with diazomethane》. The information in the text is summarized as follows:

Studies of the action of CH2N2 on barbituric acid, 1-methylbarbituric acid, and 5-ethyl-and 5-phenylbarbituric acids resulted in assignment of structures for possible positional isomers. The results came from multiple reactions, including the reaction of 6-Methoxypyrimidine-2,4(1H,3H)-dione(cas: 29458-38-6Name: 6-Methoxypyrimidine-2,4(1H,3H)-dione)

6-Methoxypyrimidine-2,4(1H,3H)-dione(cas: 29458-38-6) belongs to pyrimidine. Pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Name: 6-Methoxypyrimidine-2,4(1H,3H)-dione

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia