Category: 3764-01-0

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

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Brawn, Ryan A.; Cook, Andrew; Omoto, Kiyoyuki; Ke, Jiyuan; Karr, Craig; Colombo, Federico; Virrankoski, Milena; Prajapati, Sudeep; Reynolds, Dominic; Bolduc, David M.; Nguyen, Tuong-Vi; Gee, Patricia; Borrelli, Deanna; Caleb, Benjamin; Yao, Shihua; Irwin, Sean; Larsen, Nicholas A.; Selvaraj, Anand; Zhao, Xuesong; Ioannidis, Stephanos published their research in ACS Medicinal Chemistry Letters in 2021. The article was titled 《Discovery of Aminopyrazole Derivatives as Potent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR2 and 3》.Product Details of 3764-01-0 The article contains the following contents:

Fibroblast growth factor receptors (FGFR) 2 and 3 have been established as drivers of numerous types of cancer with multiple drugs approved or entering late stage clin. trials. A limitation of current inhibitors is vulnerability to gatekeeper resistance mutations. Using a combination of targeted high-throughput screening and structure-based drug design, we have developed a series of aminopyrazole based FGFR inhibitors that covalently target a cysteine residue on the P-loop of the kinase. The inhibitors show excellent activity against the wild-type and gatekeeper mutant versions of the enzymes. Further optimization using SAR anal. and structure-based drug design led to analogs with improved potency and drug metabolism and pharmacokinetics properties. The results came from multiple reactions, including the reaction of 2,4,6-Trichloropyrimidine(cas: 3764-01-0Product Details of 3764-01-0)

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

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2018,El-Kalyoubi, Samar A. published 《Synthesis and anticancer evaluation of some novel pyrimido[5,4-e][1,2,4]triazines and pyrazolo[3,4-d]pyrimidine using DMF-DMA as methylating and cyclizing agent》.Chemistry Central Journal published the findings.Related Products of 3764-01-0 The information in the text is summarized as follows:

A series of pyrimido[5,4-e][1,2,4]triazines I (R1 = Ph, 4-ClC6H4, 4-BrC6H4, 4-HOC6H4, 4-O2NC6H4) was obtained via condensation of 6-hydrazinyluracil with various benzaldehydes to give the hydrazones II (R2 = H) followed by nitrosation with HNO2 and intramol. cyclization. On the other hand, pyrazolopyrimidine III (R3 = 1-phenylvinyl) was obtained by the reaction of hydrazone II (R1 = Ph; R2 = Me) with DMF-DMA via formation of the intermediate IV whereas the compound III (R3 = Me) was prepared by refluxing hydrazinyluracil with DMF-DMA in DMF directly. The newly synthesized compounds I, II, III and IV were evaluated in-vitro for their anticancer activity against human lung carcinoma (A549). The compound I (R1 = 4-ClC6H4) showed the highest effect with IC50 value 3.6 μM, followed by compounds III (R3 = 1-phenylvinyl), II (R1 = R2 = H), IV, II (R1 = 4-O2NC6H4; R2 = H) and I (R1 = 4-O2NC6H4). After reading the article, we found that the author used 2,4,6-Trichloropyrimidine(cas: 3764-01-0Related Products of 3764-01-0)

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Tuning nuclear receptor selectivity of Wy14,643 towards selective retinoid X receptor modulation》 was written by Pollinger, Julius; Gellrich, Leonie; Schierle, Simone; Kilu, Whitney; Schmidt, Jurema; Kalinowsky, Lena; Ohrndorf, Julia; Kaiser, Astrid; Heering, Jan; Proschak, Ewgenij; Merk, Daniel. Electric Literature of C4HCl3N2This research focused onWy14643 retinoid x receptor pharmacokinetics. The article conveys some information:

The fatty acid sensing nuclear receptor families retinoid X receptors (RXRs) and peroxisome proliferator-activated receptors (PPARs) hold therapeutic potential in neurodegeneration. Valuable pleiotropic activities of Wy14,643 (I) in models of such conditions exceed its known PPAR agonistic profile. Here, we characterize the compound as an RXR agonist explaining the pleiotropic effects and report its systematic structure-activity relationship anal. with the discovery of specific mol. determinants driving activity on PPARs and RXRs. We have designed close analogs of the drug comprising selective and dual agonism on RXRs and PPARs that may serve as superior pharmacol. tools to study the role and interplay of the nuclear receptors in various pathologies. A systematically optimized high potency RXR agonist (II) revealed activity in vivo and active concentrations in brain. With its lack of RXR/liver X receptor-mediated side effects and superior profile compared to classical rexinoids, it establishes a new class of innovative RXR modulators to overcome key challenges in RXR targeting drug discovery. The results came from multiple reactions, including the reaction of 2,4,6-Trichloropyrimidine(cas: 3764-01-0Electric Literature of C4HCl3N2)

2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. They are generally not present in crude oils and are typically the result of additives, cleaning solutions or chemicals used for oil recovery.Electric Literature of C4HCl3N2

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 3764-01-0In 2016 ,《Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials》 appeared in Journal of Medicinal Chemistry. The author of the article were Norcross, Neil R.; Baragana, Beatriz; Wilson, Caroline; Hallyburton, Irene; Osuna-Cabello, Maria; Norval, Suzanne; Riley, Jennifer; Stojanovski, Laste; Simeons, Frederick R. C.; Porzelle, Achim; Grimaldi, Raffaella; Wittlin, Sergio; Duffy, Sandra; Avery, Vicky M.; Meister, Stephan; Sanz, Laura; Jimenez-Diaz, Belen; Angulo-Barturen, Inigo; Ferrer, Santiago; Martinez, Maria Santos; Gamo, Francisco Javier; Frearson, Julie A.; Gray, David W.; Fairlamb, Alan H.; Winzeler, Elizabeth A.; Waterson, David; Campbell, Simon F.; Willis, Paul; Read, Kevin D.; Gilbert, Ian H.. The article conveys some information:

In this paper we describe the optimization of a phenotypic hit against Plasmodium falciparum, based on a trisubstituted pyrimidine scaffold. This led to compounds with good pharmacokinetics and oral activity in a P. berghei mouse model of malaria. The most promising compound I showed a reduction in parasitemia of 96% when dosed at 30 mg/kg orally once a day for 4 days in the P. berghei mouse model of malaria. It also demonstrated a rapid rate of clearance of the erythrocytic stage of P. falciparum in the SCID mouse model with an ED90 of 11.7 mg/kg when dosed orally. Unfortunately, the compound is a potent inhibitor of cytochrome P 450 enzymes, probably due to a 4-pyridyl substituent. Nevertheless, this is a lead mol. with a potentially useful antimalarial profile, which could either be further optimized or be used for target hunting.2,4,6-Trichloropyrimidine(cas: 3764-01-0Related Products of 3764-01-0) was used in this study.

2,4,6-Trichloropyrimidine(cas: 3764-01-0) is a member of organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. They are generally not present in crude oils and are typically the result of additives, cleaning solutions or chemicals used for oil recovery.Related Products of 3764-01-0

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Jin, Xin; Piao, Hu-Ri; Pannecouque, Christophe; De Clercq, Erik; Zhuang, Chunlin; Chen, Fen-Er published an article in 2021. The article was titled 《Design of the naphthyl-diarylpyrimidines as potent non-nucleoside reverse transcriptase inhibitors (NNRTIs) via structure-based extension into the entrance channel》, and you may find the article in European Journal of Medicinal Chemistry.Application of 3764-01-0 The information in the text is summarized as follows:

A series of novel naphthyl-diarylpyrimidine (DAPY) derivatives were designed and synthesized to explore the entrance channel of the non-nucleoside reverse transcriptase inhibitors binding pocket (NNIBP) by incorporating different flexible side chains at the C-6 position. The biol. evaluation results showed that all analogs possessed promising HIV-1 inhibitory activity at the nanomolar concentration range. Three compounds (7, 9 and 39) displayed excellent potency against WT HIV-1 strain with EC50 values ranging from 5 to 10 nM and high selectivity indexes (SI = 3504, 30488 and 22846, resp.), which were higher than for nevirapine and comparable to the values for etravirine. The RT inhibition activity, preliminary structure-activity relationship and mol. docking study showed that the side chain at the C-6 position of the DAPYs occupied the entrance channel and significantly influenced anti-HIV activity and selectivity. Addnl., the physicochem. properties were investigated to evaluate the drug-like features, which indicated that introducing various substituents on the pyrimidine ring can improve solubility In the experiment, the researchers used many compounds, for example, 2,4,6-Trichloropyrimidine(cas: 3764-01-0Application of 3764-01-0)

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.Application of 3764-01-0

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2017,Korchagin, D. V.; Aldoshin, S. M.; Chernyak, A. V.; Chapyshev, S. V. published 《Molecular and crystal structure of 2,4,6-triazidopyrimidine and its chloro-substituted derivative》.Journal of Structural Chemistry published the findings.Application of 3764-01-0 The information in the text is summarized as follows:

Single-crystal X-ray diffraction combined with quantum-chem. calculations and 15N NMR spectroscopy were used to investigate the mol. and crystal structures of the high-energy 2,4,6-triazidopyrimidine and 2,4,6-triazido-5-chloropyrimidine and analyzed the dependence of the structural parameters of their azido groups on the position in the pyrimidine ring. In the experimental materials used by the author, we found 2,4,6-Trichloropyrimidine(cas: 3764-01-0Application of 3764-01-0)

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

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2016,Trist, Iuni M. L.; Nannetti, Giulio; Tintori, Cristina; Fallacara, Anna Lucia; Deodato, Davide; Mercorelli, Beatrice; Palu, Giorgio; Wijtmans, Maikel; Gospodova, Tzveta; Edink, Ewald; Verheij, Mark; de Esch, Iwan; Viteva, Lilia; Loregian, Arianna; Botta, Maurizio published 《4,6-Diphenylpyridines as Promising Novel Anti-Influenza Agents Targeting the PA-PB1 Protein-Protein Interaction: Structure-Activity Relationships Exploration with the Aid of Molecular Modeling》.Journal of Medicinal Chemistry published the findings.HPLC of Formula: 3764-01-0 The information in the text is summarized as follows:

Influenza is an infectious disease that represents an important public health burden, with high impact on the global morbidity, mortality, and economy. The poor protection and the need of annual updating of the anti-influenza vaccine, added to the rapid emergence of viral strains resistant to current therapy make the need for antiviral drugs with novel mechanisms of action compelling. In this regard, the viral RNA polymerase is an attractive target that allows the design of selective compounds with reduced risk of resistance. In previous studies we showed that the inhibition of the polymerase acidic protein-basic protein 1 (PA-PB1) interaction is a promising strategy for the development of anti-influenza agents. Starting from the previously identified 3-cyano-4,6-diphenyl-pyridines, we chem. modified this scaffold and explored its structure-activity relationships. Noncytotoxic compounds with both the ability of disrupting the PA-PB1 interaction and antiviral activity were identified, and their mechanism of target binding was clarified with mol. modeling simulations. After reading the article, we found that the author used 2,4,6-Trichloropyrimidine(cas: 3764-01-0HPLC of Formula: 3764-01-0)

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.HPLC of Formula: 3764-01-0

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2015,Delia, Thomas J.; Hood, Robin J. published 《Bromination of Pyrimidines: A Simple Inexpensive Method》.Australian Journal of Chemistry published the findings.Recommanded Product: 3764-01-0 The information in the text is summarized as follows:

Although the introduction of halogens into the pyrimidine ring has been accomplished numerous times, the methods usually involve either specialized reagents or very aggressive conditions. This communication paper describes the introduction of bromine into position 5 of the pyrimidine ring using common inorganic salts at room temperature An evaluation of the substituents required for successful reaction is provided. In the part of experimental materials, we found many familiar compounds, such as 2,4,6-Trichloropyrimidine(cas: 3764-01-0Recommanded Product: 3764-01-0)

2,4,6-Trichloropyrimidine(cas: 3764-01-0) 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.Recommanded Product: 3764-01-0

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《An efficient synthesis of designed 4-thiazolidinone fused pyrimidine derivatives as potent antimicrobial agents》 was written by Patel, Janki J.; Morja, Mayur I.; Chikhalia, Kishor H.. Name: 2,4,6-Trichloropyrimidine And the article was included in Journal of Heterocyclic Chemistry in 2020. The article conveys some information:

A novel series of hybrid 2-substituted [(pyrimidin-2-yl)hydrazinyl]thiazolidin-4-one derivatives I [R = H, 3-Cl, 4-NO2, etc.] was synthesized via aromatic nucleophilic displacement of chlorine atoms/intermol. cyclization of 2-chloro-N’-[6-morpholino-4-[(substituted-phenyl)amino]pyrimidin-2-yl]acetohydrazides II with ammonium thiocyanate. I were evaluated for their antibacterial and antifungal activities against various strains of bacteria and fungi. Structure-activity relationship and HOMO-LUMO studies were also carried out for confirming structure-biol. activity. Thus, these studies suggested that hydrazinyl pyrimidine derivatives I bearing a thiazolidinone moiety are interesting scaffolds for the development of novel antimicrobial agents. After reading the article, we found that the author used 2,4,6-Trichloropyrimidine(cas: 3764-01-0Name: 2,4,6-Trichloropyrimidine)

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.Name: 2,4,6-Trichloropyrimidine

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia