Day: October 21, 2022

《Design, Synthesis and Evaluation of Triazole-Pyrimidine Analogues as SecA Inhibitors》 was written by Cui, Jianmei; Jin, Jinshan; Chaudhary, Arpana Sagwal; Hsieh, Ying-hsin; Zhang, Hao; Dai, Chaofeng; Damera, Krishna; Chen, Weixuan; Tai, Phang C.; Wang, Binghe. Recommanded Product: 2,4,6-TrichloropyrimidineThis research focused ontriazole pyrimidine analog preparation SecA inhibitors antimicrobial resistance; SecA inhibitors; antimicrobials; protein secretion; pyrimidines; triazoles. The article conveys some information:

SecA, a key component of the bacterial Sec-dependent secretion pathway, is an attractive target for the development of new antimicrobial agents. Through a combination of virtual screening and exptl. exploration of the surrounding chem. space, we identified a hit bistriazole SecA inhibitor, SCA-21, and studied a series of analogs by systematic dissections of the core scaffold. Evaluation of these analogs allowed us to establish an initial structure-activity relationship in SecA inhibition. The best compounds in this group are potent inhibitors of SecA-dependent protein-conducting channel activity and protein translocation activity at low- to sub-micromolar concentrations They also have minimal inhibitory concentration (MIC) values against various strains of bacteria that correlate well with the SecA and protein translocation inhibition data. These compounds are effective against methicillin-resistant Staphylococcus aureus strains with various levels of efflux pump activity, indicating the capacity of SecA inhibitors to null the effect of multidrug resistance. Results from studies of drug-affinity-responsive target stability and protein pull-down assays are consistent with SecA as a target for these compounds The experimental part of the paper was very detailed, including the reaction process of 2,4,6-Trichloropyrimidine(cas: 3764-01-0Recommanded Product: 2,4,6-Trichloropyrimidine)

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.Recommanded Product: 2,4,6-Trichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2016,Sabat, Nazarii; Naus, Petr; Matyasovsky, Jan; Dziuba, Dmytro; Slavetinska, Lenka Postova; Hocek, Michal published 《Synthesis of fluorescent 2-substituted 6-(Het)aryl-7-deazapurine bases {4-(Het)aryl-pyrrolo[2,3-d]pyrimidines} by aqueous Suzuki-Miyaura cross-coupling reactions》.Synthesis published the findings.Quality Control of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine The information in the text is summarized as follows:

A series of 4-(het)aryl-pyrrolo[2,3-d]pyrimidines [6-(het)aryl-7-deazapurine bases] bearing a H, NH2, CH3, F, or Cl group at the 2-position and either H or F at the 5-position (position 7 of 7-deazapurine) were prepared in a single step by the aqueous Suzuki-Miyaura cross-coupling reactions of the corresponding 6-chloro-7-deazapurines with (het)arylboronic acids. Unlike their ribonucleoside derivatives, which are potent cytostatics, the deazapurine bases did not show significant biol. activity but most of them exerted bright fluorescence with emission maxima 368-468 nm and high quantum yields up to 0.83. In the experimental materials used by the author, we found 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Quality Control of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine)

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. Quality Control of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Huang, Chen-Song; Xu, Qiong-Cong; Dai, Chunlei; Wang, Liying; Tien, Yi-Chih; Li, Fuxi; Su, Qiao; Huang, Xi-Tai; Wu, Jun; Zhao, Wei; Yin, Xiao-Yu published an article in 2021. The article was titled 《Nanomaterial-Facilitated Cyclin-Dependent Kinase 7 Inhibition Suppresses Gallbladder Cancer Progression via Targeting Transcriptional Addiction》, and you may find the article in ACS Nano.Reference of 2,4,6-Trichloropyrimidine The information in the text is summarized as follows:

Gallbladder cancer (GBC) is the most aggressive malignancy of the biliary tract cancer, and there is a lack of effective treatment. Here, we developed a nanoparticle platform (8P4 NP) that can deliver THZ1, a cyclin-dependent kinase 7 (CDK7) inhibitor, to treat GBC. Anal. of datasets demonstrated that CDK7 was pos. correlated with poor prognosis. CDK7 inhibition suppressed cell proliferation, induced apoptosis, and caused cell cycle block in GBC cells. THZ1 downregulated CDK7-mediated phosphorylation of RNA polymerase II (RNAPII), resulting in a significant downregulation of transcriptional programs, with a preferential repression of oncogenic transcription factors. To improve the tumor targeting efficiency of THZ1, 8P4 NPs were prepared and assembled with THZ1 to form THZ1@8P4 NPs. Compared with free THZ1, THZ1@8P4 NPs showed more advantages in prolonging blood circulation, escaping from lysosomes and increasing cellular uptake. Importantly, THZ1@8P4 NPs demonstrated a more significant inhibition effect on GBC cells than free THZ1 in vitro. In addition, THZ1@8P4 NPs could efficiently deliver THZ1 to tumor sites in a patient-derived xenograft model of early recurrence, leading to tumor regression and transcriptional inhibition with minimal toxicity. In summary, we conclude that THZ1@8P4 NPs provide a potent therapeutic strategy that targets CDK7-mediated transcriptional addiction in GBC.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

Category: pyrimidinesIn 2021 ,《Synthesis of Luminescent Fused Imidazole Bicyclic Acetic Esters by a Multicomponent Palladium Iodide-Catalyzed Oxidative Alkoxycarbonylation Approach》 appeared in ChemCatChem. The author of the article were Veltri, Lucia; Prestia, Tommaso; Russo, Patrizio; Clementi, Catia; Vitale, Paola; Ortica, Fausto; Gabriele, Bartolo. The article conveys some information:

A new multicomponent catalytic approach to important fused imidazole bicyclic acetic esters, whose core is present in many biol. active principles, is presented. It is based on the sequential cyclization-alkoxycarbonylation-isomerization of readily available N-heterocyclic propargylamine derivatives, carried out under oxidative conditions using a simple catalytic system consisting of PdI2 (1 mol%) in conjunction with KI (1 equivalent), in the presence of AcONa as additive (1 equivalent) at 100°C under 20 bar of a 4 : 1 mixture CO-air. Under the optimized conditions, several N-(prop-2-yn-1-yl)pyridin-2-amines were smoothly converted into alkyl 2-(imidazo[1,2-a]pyridin-3-yl)acetates in fair yields (51-77%). The method was also applied to the conversion of N-(prop-2-yn-1-yl)pyrimidin-2-amine into 2-(imidazo[1,2-a]pyrimidin-3-yl)acetate and of N-(prop-2-yn-1-yl)pyrazin-2-amine into 2-(imidazo[1,2-a]pyrazin-3-yl)acetate. Some of the newly synthesized bicyclic derivatives have shown promising luminescence properties. The experimental part of the paper was very detailed, including the reaction process of 2,4,6-Trichloropyrimidine(cas: 3764-01-0Category: pyrimidines)

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.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2018,ChemistrySelect included an article by Xiao, Ke; Zhu, Congjun; Lin, Maohua; Song, Chuanjun; Chang, Junbiao. Formula: C8H10N2O2. The article was titled 《Base-Promoted Cycloisomerization for the Synthesis of Indolizines and Related Heterocycles》. The information in the text is summarized as follows:

The base-mediated 5-exo-dig type cyclization reaction of homopropargyl pyridines for the construction of indolizines I (R1= COOEt, CN, COMe, etc.; R2 = Me, CH2C6H4, 4-ClC6H4CH2, 4-MeOC6H4CH2; R3 = H, 7-Me) has been reported for the first time. A variety of indolizine derivatives could be obtained in moderate to excellent isolated yields by treatment of homopropargyl pryidines with cesium carbonate in DMSO at 100°. This strategy could also be adapted to the synthesis of pyrrolo[1,2-a]quinolines and pyrrolo[1,2-a]pyrimidines from the corresponding homopropargyl quinolines and homopropargyl pyrimidines, resp. The mechanism involves α C-H deprotonation, 5-exo-dig cyclization, and isomerization of the exocyclic double bond to provide the heteroaromatic system. The transformation reported herein does not require the aid of transition metal catalysts or halogens, and is thus environmentally friendly. In the part of experimental materials, we found many familiar compounds, such as Ethyl 2-(pyrimidin-2-yl)acetate(cas: 63155-11-3Formula: C8H10N2O2)

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.Formula: C8H10N2O2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2018,Bucevicius, Jonas; Turks, Maris; Tumkevicius, Sigitas published 《Easy Access to Isomeric 7-Deazapurine-1,2,3-Triazole Conjugates via S N Ar and CuAAC Reactions of 2,6-Diazido-7-deazapurines》.Synlett published the findings.Synthetic Route of C6H3Cl2N3 The information in the text is summarized as follows:

A simple and efficient synthesis of isomeric 7-deazapurine-1,2,3-triazole conjugates, e.g. I, with amino substituents from readily available 9-alkyl-2,6-diazido-7-deazapurines has been developed using consecutive CuAAC and regioselective nucleophilic substitution reactions of azido and 1,2,3-triazole groups with amines. The experimental part of the paper was very detailed, including the reaction process of 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Synthetic Route of C6H3Cl2N3)

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. Synthetic Route of C6H3Cl2N3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2018,Molecules included an article by Wright, Emily W.; Nelson, Ronald A. Jr.; Karpova, Yelena; Kulik, George; Welker, Mark E.. COA of Formula: C4HCl3N2. The article was titled 《Synthesis and PI3 kinase inhibition activity of some novel trisubstituted morpholinopyrimidines》. The information in the text is summarized as follows:

A number of new substituted morpholinopyrimidines were prepared utilizing sequential nucleophilic aromatic substitution and cross-coupling reactions. One of the disubstituted pyrimidines was converted into two trisubstituted compounds which were screened as PI3K inhibitors relative to the well-characterized PI3K inhibitor ZSTK474, and were found to be 1.5-3-times more potent. A leucine linker was attached to the most active inhibitor since it would remain on any peptide-containing prodrug after cleavage by prostate-specific antigen, and it did not prevent inhibition of AKT phosphorylation and hence the inhibition of PI3K by the modified inhibitor. The experimental part of the paper was very detailed, including the reaction process of 2,4,6-Trichloropyrimidine(cas: 3764-01-0COA of Formula: C4HCl3N2)

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.COA of Formula: C4HCl3N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Zhang, Yiwen; Zhang, Min; Han, Zhengbo; Huang, Shijun; Yuan, Daqiang; Su, Weiping published an article in 2021. The article was titled 《Atmosphere-Pressure Methane Oxidation to Methyl Trifluoroacetate Enabled by a Porous Organic Polymer-Supported Single-Site Palladium Catalyst》, and you may find the article in ACS Catalysis.Recommanded Product: 1193-21-1 The information in the text is summarized as follows:

The efficient conversion of methane into methanol at low temperature under low pressure remains a great challenge largely because of the inertness and poor solubility of methane. Herein, we report that a porous organic polymer-supported Pd catalyst, which was constructed via Friedel-Crafts type polymerization between 4,6-dichloropyrimidine and 1,3,5-tri-Ph benzene and subsequent metalation, enabled the conversion of methane to Me trifluoroacetate, a precursor to methanol, under atm. pressure (1 atm) at 80°C to afford a 51% yield relative to methane with a TON of 664 over 20 h. On increasing the pressure to 30 bar, this palladium catalyst offered a TON of 1276 for a run and could be reused for at least five runs without a notable loss of activity. The characterization of this Pd catalyst revealed its good affinity for methane uptake that would increase the concentration of methane in the local space around the Pd center and the homogeneous distribution of Pd2+ on support that would protect the catalytically active metal species, shedding light on the high catalytic activity of this Pd catalyst toward methane conversion. The experimental process involved the reaction of 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

Related Products of 3934-20-1In 2022 ,《Pyrimidyn-Based Dynamin Inhibitors as Novel Cytotoxic Agents》 appeared in ChemMedChem. The author of the article were Odell, Luke R.; Chau, Ngoc; Russell, Cecilia C.; Young, Kelly A.; Gilbert, Jayne; Robinson, Phillip J.; Sakoff, Jennette A.; McCluskey, Adam. The article conveys some information:

Five focused libraries of pyrimidine-based dynamin GTPase inhibitors, in total 69 compounds were synthesized, and their dynamin inhibition and broad-spectrum cytotoxicity examined Dynamin plays a crucial role in mitosis, and as such inhibition of dynamin was expected to broadly correlate with the observed cytotoxicity. The pyrimidines synthesized ranged from mono-substituted to trisubstituted. The highest levels of dynamin inhibition were noted with di- and tri- substituted pyrimidines, especially those with pendent amino alkyl chains. Short chains and simple heterocyclic rings reduced dynamin activity. There were three levels of dynamin activity noted: 1-10, 10-25 and 25-60 μM. Screening of these compounds in a panel of cancer cell lines: SW480 (colon), HT29 (colon), SMA (spontaneous murine astrocytoma), MCF-7 (breast), BE2-C (glioblastoma), SJ-G2 (neuroblastoma), MIA (pancreas), A2780 (ovarian), A431 (skin), H460 (lung), U87 (glioblastoma) and DU145 (prostate) cell lines reveal a good correlation between the observed dynamin inhibition and the observed cytotoxicity. The most active analogs (31 a,b) developed returned average GI50 values of 1.0 and 0.78 μM across the twelve cell lines examined These active analogs were: N2-(3-dimethylaminopropyl)-N4-dodecyl-6-methylpyrimidine-2,4-diamine (31 a) and N4-(3-dimethylaminopropyl)-N2-dodecyl-6-methylpyrimidine-2,4-diamine (31 b). The experimental part of the paper was very detailed, including the reaction process of 2,4-Dichloropyrimidine(cas: 3934-20-1Related Products of 3934-20-1)

2,4-Dichloropyrimidine(cas: 3934-20-1) 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.Related Products of 3934-20-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Electric Literature of C6H3Cl2N3In 2015 ,《2,4-diazidopyrrolo[2,3-d]pyrimidines: synthesis, ring-chain tautomerism and Cu(I)-catalyzed azide-alkyne cycloaddition reaction》 was published in Chemija. The article was written by Bucevicius, Jonas; Tumkevicius, Sigitas. The article contains the following contents:

2,4-Diazidopyrrolo[2,3-d]pyrimidines were synthesized by the reaction of the corresponding 2,4-dichloropyrrolo[2,3-d]pyrimidines with sodium azide at room temperature 2,4-Diazidopyrrolo[2,3-d]pyrimidines were exist in an equilibrium with the corresponding 5-azidopyrrolo[3,2-e]tetrazolo[1,5-c]pyrimidine. The proportion of the tetrazole tautomer increases with increasing solvent polarity. The CuAAC reaction of the obtained azides with 3-methylphenyl- and 4-biphenylylethynes afforded the corresponding 2,4-bis(4-aryl-1,2,3-triazol-1-yl)pyrrolo[2,3-d]pyrimidines.2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Electric Literature of C6H3Cl2N3) was used in this study.

2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4) belongs to pyrimidine. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own. Electric Literature of C6H3Cl2N3They 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