Day: October 13, 2022

Safety of 4,6-DichloropyrimidineIn 2019 ,《Synthesis, pharmacological characterization, and structure-activity relationships of non-canonical selective agonists for α7 nAChRs》 appeared in Journal of Medicinal Chemistry. The author of the article were Camacho-Hernandez, Gisela Andrea; Stokes, Clare; Duggan, Brendan M.; Kaczanowska, Katarzyna; Brandao-Araiza, Stefania; Doan, Lisa; Papke, Roger L.; Taylor, Palmer. The article conveys some information:

Noncanonical 2,4,6-substituted pyrimidine analogs were prepared for a structure-activity relationship study. The new lead compounds activate selectively the α7 nAChRs with EC50’s between 30-140 nM in a PNU-120596-dependent, cell-based calcium influx assay. After characterizing the expanded lead landscape, author ranked the compounds for rapid activation using Xenopus oocytes expressing human α7 nAChR with a two-electrode voltage clamp. This approach enabled us to define the mol. determinants governing rapid activation, agonist potency, and desensitization of α7 nAChRs after exposure to pyrimidine analogs, thereby distinguishing this subclass of non-canonical agonists from previously defined types of agonists (agonists, partial agonists, silent agonists, and ago-PAMs). By NMR, author analyzed pKa values for ionization of lead candidates, demonstrating distinctive modes of interaction for this landscape of ligands. In the experiment, the researchers used 4,6-Dichloropyrimidine(cas: 1193-21-1Safety of 4,6-Dichloropyrimidine)

4,6-Dichloropyrimidine(cas: 1193-21-1) 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.Safety of 4,6-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Calderwood, David J.; Johnston, David N.; Munschauer, Rainer; Rafferty, Paul published an article in Bioorganic & Medicinal Chemistry Letters. The title of the article was 《Pyrrolo[2,3-d]pyrimidines containing diverse N-7 substituents as potent inhibitors of Lck》.Recommanded Product: 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine The author mentioned the following in the article:

A series of pyrrolo[2,3-d]pyrimidines was synthesized and structure-activity relationship was evaluated as inhibitors of Lck. Lck accommodates a diverse set of substituents at N-7. Altering the substituent at N-7 provided another compound, an orally available lck inhibitor which inhibited TCR mediated IL-2 production after oral dosing. In the experiment, the researchers used 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8Recommanded Product: 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine)

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.Recommanded Product: 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2016,Michellys, Pierre-Yves; Chen, Bei; Jiang, Tao; Jin, Yunho; Lu, Wenshuo; Marsilje, Thomas H.; Pei, Wei; Uno, Tetsuo; Zhu, Xuefeng; Wu, Baogen; Nguyen, Truc Ngoc; Bursulaya, Badry; Lee, Christian; Li, Nanxin; Kim, Sungjoon; Tuntland, Tove; Liu, Bo; Sun, Frank; Steffy, Auzon; Hood, Tami published 《Design and synthesis of novel selective anaplastic lymphoma kinase inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.Quality Control of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine The information in the text is summarized as follows:

Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase belonging to the insulin receptor superfamily. Expression of ALK in normal human tissues is only found in a subset of neural cells, however it is involved in the genesis of several cancers through genetic aberrations involving translocation of the kinase domain with multiple fusion partners (e.g., NPM-ALK in anaplastic large cell lymphoma ALCL or EML4-ALK in non-small cell lung cancer) or activating mutations in the full-length receptor resulting in ligand-independent constitutive activation (e.g., neuroblastoma). Here we are reporting the discovery of novel and selective anaplastic lymphoma kinase inhibitors from specific modifications of the 2,4-diaminopyridine core present in TAE684 and LDK378. Synthesis, structure activity relationships (SAR), absorption, distribution, metabolism, and excretion (ADME) profile, and in vivo efficacy in a mouse xenograft model of anaplastic large cell lymphoma are described. In addition to this study using 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine, there are many other studies that have used 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Quality Control of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine) was used in this study.

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

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Quality Control of 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amineOn September 30, 2012 ,《Use of kinase inhibitors to correct ΔF508-CFTR function》 was published in Molecular and Cellular Proteomics. The article was written by Trzcinska-Daneluti, Agata M.; Nguyen, Leo; Jiang, Chong; Fladd, Christopher; Uehling, David; Prakesch, Michael; Al-Awar, Rima; Rotin, Daniela. The article contains the following contents:

The most common mutation in cystic fibrosis (CF) is a deletion of Phe at position 508 (ΔF508-CFTR). ΔF508-CFTR is a trafficking mutant that is retained in the ER, unable to reach the plasma membrane. To identify compounds and drugs that rescue this trafficking defect, we screened a kinase inhibitor library enriched for small mols. already in the clinic or in clin. trials for the treatment of cancer and inflammation, using our recently developed high-content screen technol. The top hits of the screen were further validated by (1) biochem. anal. to demonstrate the presence of mature (Band C) ΔF508-CFTR, (2) flow cytometry to reveal the presence of ΔF508-CFTR at the cell surface, (3) short-circuit current (Isc) anal. in Ussing chambers to show restoration of function of the rescued ΔF508-CFTR in epithelial MDCK cells stably expressing this mutant (including EC50 determinations), and importantly (4) Isc anal. of Human Bronchial Epithelial (HBE) cells harvested from homozygote ΔF508-CFTR transplant patients. Interestingly, several inhibitors of receptor Tyr kinases (RTKs), such as SU5402 and SU6668 (which target FGFRs, VEGFR, and PDGFR) exhibited strong rescue of ΔF508-CFTR, as did several inhibitors of the Ras/Raf/MEK/ERK or p38 pathways (e.g. (5Z)-7-oxozeaenol). Prominent rescue was also observed by inhibitors of GSK-3β (e.g. GSK-3β Inhibitor II and Kenpaullone). These results identify several kinase inhibitors that can rescue ΔF508-CFTR to various degrees, and suggest that use of compounds or drugs already in the clinic or in clin. trials for other diseases can expedite delivery of treatment for CF patients. The experimental part of the paper was very detailed, including the reaction process of 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine(cas: 213743-31-8Quality Control of 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine)

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. Quality Control of 7-Cyclopentyl-5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Quality Control of 4-Chloro-6-(4-(trifluoromethyl)phenyl)pyrimidineOn March 15, 2008, Doherty, Elizabeth M.; Retz, Daniel; Gavva, Narender R.; Tamir, Rami; Treanor, James J. S.; Norman, Mark H. published an article in Bioorganic & Medicinal Chemistry Letters. The article was 《4-Aminopyrimidine tetrahydronaphthols: A series of novel vanilloid receptor-1 antagonists with improved solubility properties》. The article mentions the following:

8-{6-[4-(Trifluoromethyl)phenyl]pyrimidin-4-ylamino}-1,2,3,4-tetrahydronaphthalen-2-ol and its analogs were shown to be potent inhibitors of human and rat TRPV1 in vitro with increased solubility Synthesis, SAR, and improvements in metabolic stability and absorption of these compounds are described. The experimental process involved the reaction of 4-Chloro-6-(4-(trifluoromethyl)phenyl)pyrimidine(cas: 659729-09-6Quality Control of 4-Chloro-6-(4-(trifluoromethyl)phenyl)pyrimidine)

4-Chloro-6-(4-(trifluoromethyl)phenyl)pyrimidine(cas: 659729-09-6) belongs to pyrimidine. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own. Quality Control of 4-Chloro-6-(4-(trifluoromethyl)phenyl)pyrimidineThey have been used in a wide variety of pharmaceuticals including general anesthetics, anti-epilepsy medication, anti-malaria medication, drugs for treating high blood pressure, and HIV medication.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Atkinson, Benjamin N.; Steadman, David; Mahy, William; Zhao, Yuguang; Sipthorp, James; Bayle, Elliott D.; Svensson, Fredrik; Papageorgiou, George; Jeganathan, Fiona; Frew, Sarah; Monaghan, Amy; Bictash, Magda; Jones, E. Yvonne; Fish, Paul V. published an article on February 1 ,2020. The article was titled 《Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.SDS of cas: 108831-66-9 The information in the text is summarized as follows:

The carboxylesterase Notum is a key neg. regulator of the Wnt signaling pathway by mediating the depalmitoleoylation of Wnt proteins. Our objective was to discover potent small mol. inhibitors of Notum suitable for exploring the regulation of Wnt signaling in the central nervous system. Scaffold-hopping from thienopyrimidine acids 1 and 2, supported by X-ray structure determination, identified 3-methylimidazolin-4-one amides 20-24 as potent inhibitors of Notum with activity across three orthogonal assay formats (biochem., extra-cellular, occupancy). A preferred example 24 demonstrated good stability in mouse microsomes and plasma, and cell permeability in the MDCK-MDR1 assay albeit with modest P-gp mediated efflux. Pharmacokinetic studies with 24 were performed in vivo in mouse with single oral administration of 24 showing good plasma exposure and reasonable CNS penetration. We propose that 24 is a new chem. tool suitable for cellular studies to explore the fundamental biol. of Notum. In the experiment, the researchers used many compounds, for example, 6-Methyl-3H-thieno[2,3-d]pyrimidin-4-one(cas: 108831-66-9SDS of cas: 108831-66-9)

6-Methyl-3H-thieno[2,3-d]pyrimidin-4-one(cas: 108831-66-9) 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.SDS of cas: 108831-66-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Lefebvre, Carole-Anne; Forcellini, Elsa; Boutin, Sophie; Cote, Marie-France; C.-Gaudreault, Rene; Mathieu, Patrick; Lague, Patrick; Paquin, Jean-Francois published an article on January 15 ,2017. The article was titled 《Synthesis of novel substituted pyrimidine derivatives bearing a sulfamide group and their in vitro cancer growth inhibition activity》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Name: 4-Chloro-6-(4-(trifluoromethyl)phenyl)pyrimidine The information in the text is summarized as follows:

The synthesis of two series of novel substituted pyrimidine derivatives bearing a sulfamide group have been described and their in vitro cancer growth inhibition activities have been evaluated against three human tumor cell lines (HT-29, M21, and MCF7). In general, growth inhibition activity has been enhanced by the introduction of a bulky substituent on the aromatic ring with the best compound having GI50 < 6 μM for all the human tumor cell lines. The MCF7 selective compounds were evaluated on four addnl. human invasive breast ductal carcinoma cell lines (MDA-MB-231, MDA-MB-468, SKBR3, and T47D) and were selective against T47D cell line in all cases except one, suggesting a potential antiestrogen activity. In addition to this study using 4-Chloro-6-(4-(trifluoromethyl)phenyl)pyrimidine, there are many other studies that have used 4-Chloro-6-(4-(trifluoromethyl)phenyl)pyrimidine(cas: 659729-09-6Name: 4-Chloro-6-(4-(trifluoromethyl)phenyl)pyrimidine) was used in this study.

4-Chloro-6-(4-(trifluoromethyl)phenyl)pyrimidine(cas: 659729-09-6) belongs to pyrimidine. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own. Name: 4-Chloro-6-(4-(trifluoromethyl)phenyl)pyrimidineThey have been used in a wide variety of pharmaceuticals including general anesthetics, anti-epilepsy medication, anti-malaria medication, drugs for treating high blood pressure, and HIV medication.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《5-Nitro-2,4-dichloropyrimidine as an universal model for low-energy electron processes relevant for radiosensitization》 was written by Luxford, Thomas F. M.; Pshenichnyuk, Stanislav A.; Asfandiarov, Nail L.; Perecko, Tomas; Falk, Martin; Kocisek, Jaroslav. Recommanded Product: 3934-20-1 And the article was included in International Journal of Molecular Sciences in 2020. The article conveys some information:

We report exptl. results of low-energy electron interactions with 5-nitro-2,4- dichloropyrimidine isolated in the gas phase and hydrated in a cluster environment. The mol. exhibits a very rare combination of many so far hypothesized low-energy electron induced mechanisms, which may be responsible for synergism in concurrent chemo-radiation therapy of cancer. In contrast to many previous efforts to design an ideal radiosensitizer based on one mode of action, the present model mol. presents an alternative approach, where several modes of action are combined. With respect to the processes induced by the low-energy electrons, this is not a trivial task because of strong bond specificity of the dissociative electron attachment reaction, as it is discussed in the present paper. Unfortunately, low solubility and high toxicity of the mol., as obtained from preliminary MTT assay tests, do not enable further studies of its activity in real biol. systems but it can advantageously serve as a model or a base for rational design of radiosensitizers. The results came from multiple reactions, including the reaction 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

The author of 《Synthesis and Spectral Characterization of New Bis(2-(pyrimidin-2-yl)ethoxy)alkanes and Their Pharmacological Activity》 were Rani, Vangavaragu Jhansi; Aminedi, Raghavendra; Polireddy, Kishore; Jagadeeswarareddy, Kanala. And the article was published in Archiv der Pharmazie (Weinheim, Germany) in 2012. Name: Ethyl 2-(pyrimidin-2-yl)acetate The author mentioned the following in the article:

The pyrimidine nucleus is an important component of nucleic acids (DNA and RNA) and vitamins (B2 and folic acid). It is evident from the literature that pyrimidine derivatives possess a wide spectrum of biol. activities such as antioxidant, anticancer, antibacterial, and anti-inflammatory activities. On the basis of diverse biol. activities, the authors attempted to synthesize a series of novel bis(2-(pyrimidin-2-yl)ethoxy)alkanes 5a-j in four steps with good yields. 2-Chloropyrimidine (1) was reacted with di-Et malonate in the presence of sodium hydride in dry DMF to yield the intermediate di-Et 2-(pyrimidin-2-yl)malonate (2), which on further reaction with sodium chloride and DMSO yielded Et 2-(pyrimidin-2-yl)ethanoate (3). Reduction with sodium borohydride (NaBH4) resulted in the formation of 2-(pyrimidin-2-yl)ethanol (4). This was further reacted with various dibromoalkanes to obtain the title compounds 5a-j. Next, the authors evaluated the antioxidant properties of the title compounds using four in vitro test systems: the 2,2-diphenyl-2-picrylhydrazyl radical-, superoxide radical-, and hydroxyl radical-scavenging assays, and the anti-lipid peroxidation activity test. The title compounds showed promising antioxidant activity when compared to butylated hydroxytoluene. The potency of their antioxidant activity was mainly influenced by the alkyl fragment attached to 2-(pyrimidin-2-yl)ethanol. The Et and Bu fragments linked to oxygen led to increased antioxidant activity of the title compounds (i.e., 5b and 5d) in all the in vitro assays. The results came from multiple reactions, including the reaction of Ethyl 2-(pyrimidin-2-yl)acetate(cas: 63155-11-3Name: Ethyl 2-(pyrimidin-2-yl)acetate)

Ethyl 2-(pyrimidin-2-yl)acetate(cas: 63155-11-3) is a member of pyrimidine. Pyrimidine derivatives are an important class of N-heterocycles. They are well-known for their wide spectrum of promising biological activities such as antitumors, bactericidals, and fungicidal.Name: Ethyl 2-(pyrimidin-2-yl)acetate

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

COA of Formula: C6H7N3O2SOn March 1, 2005, Du, Miao; Jiang, Xiu-Juan; Zhao, Xiao-Jun published an article in Acta Crystallographica, Section E: Structure Reports Online. The article was 《Diaquabis(2,5-di-3-pyridyl-1,3,4-oxadiazole)dithiocyanatomanganese(II): a three-dimensional supramolecular network formed through O-H···N and C-H···S interactions》. The article mentions the following:

Crystals of the neutral mononuclear title complex are triclinic, space group P1̅, with a 8.1951(19), b 8.762(2), c 10.619(3) Å, α 82.472(3), β 77.181(3), γ 79.873(3)°; Z = 1, dc = 1.494; R = 0.035, w(F2) = 0.099 for 2540 reflections. The structure is centrosym.; the MnII atom lies on an inversion center and is six-coordinate (MnN4O2), with an octahedral geometry comprising two trans monodentate 2,5-di-3-pyridyl-1,3,4-oxadiazole ligands, two thiocyanate ligands and two bound H2O mols. Intermol. O-H···N H bonds between these monomeric units result in two-dimensional supramol. layers with a parallel arrangement, which are stabilized by intralayer aromatic stacking and further extended to a three-dimensional network via interlayer weak C-H···S interactions. The results came from multiple reactions, including the reaction of 4-Amino-2-(methylthio)pyrimidine-5-carboxylic acid(cas: 771-81-3COA of Formula: C6H7N3O2S)

4-Amino-2-(methylthio)pyrimidine-5-carboxylic acid(cas: 771-81-3) belongs to anime. Left-handed and right-handed forms (mirror-image configurations, known as optical isomers or enantiomers) are possible when all the substituents on the central nitrogen atom are different (i.e., the nitrogen is chiral). With amines, there is extremely rapid inversion in which the two configurations are interconverted.COA of Formula: C6H7N3O2S

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia