Day: October 20, 2022

In 2019,Journal of Medicinal Chemistry included an article by Liang, Xiaofei; Wang, Beilei; Chen, Cheng; Wang, Aoli; Hu, Chen; Zou, Fengming; Yu, Kailin; Liu, Qingwang; Li, Feng; Hu, Zhenquan; Lu, Tingting; Wang, Junjie; Wang, Li; Weisberg, Ellen L.; Li, Lili; Xia, Ruixiang; Wang, Wenchao; Ren, Tao; Ge, Jian; Liu, Jing; Liu, Qingsong. Related Products of 1193-21-1. The article was titled 《Discovery of N-(4-(6-acetamidopyrimidin-4-yloxy)phenyl)-2-(2-(trifluoromethyl)phenyl)acetamide (CHMFL-FLT3-335) as a potent FMS-like tyrosine kinase 3 internal tandem duplication (FLT3-ITD) mutant selective inhibitor for acute myeloid leukemia》. The information in the text is summarized as follows:

Most of the current FMS-like tyrosine kinase 3 (FLT3) inhibitors lack selectivity between FLT3 kinase and cKIT kinase as well as the FLT3 wt and internal tandem duplication (ITD) mutants. We report a new compound I, which displays GI50 values of 30-80 nM against different ITD mutants and achieves selectivity over both FLT3 wt (8-fold) and cKIT kinase in the transformed BaF3 cells (>300-fold). I potently inhibits the proliferation of the FLT3-ITD-pos. acute myeloid leukemia cancer lines through suppression of the phosphorylation of FLT3 kinase and downstream signaling pathways, induction of apoptosis, and arresting the cell cycle into the G0/G1 phase. I also displays potent antiproliferative effect against FLT3-ITD-pos. patient primary cells, whereas it does not apparently affect FLT3 wt primary cells. In addition, it also exhibits a good therapeutic window to PBMC compared to PKC412. In the in vivo studies, I demonstrates favorable PK profiles and suppresses the tumor growth in the MV4-11 cell inoculated mouse xenograft model. In the experimental materials used by the author, we found 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. Almost all organochlorine compounds are synthesized. It is widely used as intermediates, solvents and pesticides of chemical synthetic products.Related Products of 1193-21-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The author of 《(S)-4-(Difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530), a Potent, Orally Bioavailable, and Brain-Penetrable Dual Inhibitor of Class I PI3K and mTOR Kinase》 were Rageot, Denise; Bohnacker, Thomas; Keles, Erhan; McPhail, Jacob A.; Hoffmann, Reece M.; Melone, Anna; Borsari, Chiara; Sriramaratnam, Rohitha; Sele, Alexander M.; Beaufils, Florent; Hebeisen, Paul; Fabbro, Doriano; Hillmann, Petra; Burke, John E.; Wymann, Matthias P.. And the article was published in Journal of Medicinal Chemistry in 2019. Reference of 2,4,6-Trichloropyrimidine The author mentioned the following in the article:

The phosphoinositide 3-kinase (PI3K)/mechanistic target of rapamycin (mTOR) pathway is frequently overactivated in cancer, and drives cell growth, proliferation, survival, and metastasis. Here, we report a structure-activity relationship study, which led to the discovery of a drug-like ATP-site PI3K/mTOR kinase inhibitor: (S)-4-(difluoromethyl)-5-(4-(3-methylmorpholino)-6-morpholino-1,3,5-triazin-2-yl)pyridin-2-amine (PQR530, compound 6), which qualifies as a clin. candidate due to its potency and specificity for PI3K and mTOR kinases, and its pharmacokinetic properties, including brain penetration. Compound 6 showed excellent selectivity over a wide panel of kinases and an excellent selectivity against unrelated receptor enzymes and ion channels. Moreover, compound 6 prevented cell growth in a cancer cell line panel. The preclin. in vivo characterization of compound 6 in an OVCAR-3 xenograft model demonstrated good oral bioavailability, excellent brain penetration, and efficacy. Initial toxicity studies in rats and dogs qualify 6 for further development as a therapeutic agent in oncol. In addition to this study using 2,4,6-Trichloropyrimidine, there are many other studies that have used 2,4,6-Trichloropyrimidine(cas: 3764-01-0Reference of 2,4,6-Trichloropyrimidine) was used in this study.

2,4,6-Trichloropyrimidine(cas: 3764-01-0) 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.Reference of 2,4,6-Trichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Nature-Inspired (di)Azine-Bridged Bisindole Alkaloids with Potent Antibacterial In Vitro and In Vivo Efficacy against Methicillin-Resistant Staphylococcus aureus》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Rehberg, Nidja; Sommer, Gereon A.; Driessen, Daniel; Kruppa, Marco; Adeniyi, Emmanuel T.; Chen, Shang; Wang, Lin; Wolf, Karina; Tasch, Boris O. A.; Ioerger, Thomas R.; Zhu, Kui; Mueller, Thomas J. J.; Kalscheuer, Rainer. Computed Properties of C4H2Cl2N2 The article mentions the following:

Natural bisindole alkaloids such as Hyrtinadine A and Alocasin A, which are known to exhibit diverse bioactivities, provide promising chem. scaffolds for drug development. By optimizing the Masuda borylation-Suzuki coupling sequence, a library of various natural product-derived and non-natural (di)azine-bridged bisindoles was created. While unsubstituted bisindoles were devoid of antibacterial activity, 5,5′-chloro derivatives were highly active against methicillin-resistant Staphylococcus aureus (MRSA) and further Gram-pos. pathogens at minimal inhibitory concentrations ranging from 0.20 to 0.78μM. These compounds showed strong bactericidal killing effects but only moderate cytotoxicity against human cell lines. Furthermore, the two front-runner compounds 4j and 4n exhibited potent in vivo efficacy against MRSA in a mouse wound infection model. Although structurally related bisindoles were reported to specifically target pyruvate kinase in MRSA, antibacterial activity of 4j and 4n is independent of pyruvate kinase. Rather, these compounds lead to bacterial membrane permeabilization and cellular efflux of low-mol.-weight mols. The experimental process involved the reaction of 2,4-Dichloropyrimidine(cas: 3934-20-1Computed Properties of C4H2Cl2N2)

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.Computed Properties of C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《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