Tag: 100-200

Ding, Shi; Dong, Xiaoyong; Gao, Ziye; Zheng, Xiangshan; Ji, Jingchao; Zhang, Mingjuan; Liu, Fang; Wu, Shuang; Li, Min; Song, Wenshan; Shen, Jiwei; Duan, Wenwen; Liu, Ju; Chen, Ye published an article in 2022. The article was titled 《Design, synthesis and biological evaluation of novel N-(3-amino-4-methoxyphenyl)acrylamide derivatives as selective EGFRL858R/T790M kinase inhibitors》, and you may find the article in Bioorganic Chemistry.Reference of 2,4-Dichloropyrimidine The information in the text is summarized as follows:

On the basis of N-(3-amino-4-methoxyphenyl)acrylamide scaffold, a series of novel compounds containing 3-substitutional-1-methyl-1H-indole, 2-substitutional pyrrole or thiophene moieties were synthesized and their in vitro antiproliferation activities against A549 and H1975 cell lines were evaluated. The results indicated that most of the compounds showed moderate to excellent antitumor activities. Especially, compounds 9a (A549 IC50 = 1.96 μM, H1975 IC50 = 0.095 μM), 17i (A549 IC50 = 4.17 μM, H1975 IC50 = 0.052 μM), 17j (A549 IC50 = 1.67 μM, H1975 IC50 = 0.061 μM) exhibited comparable antitumor activities and selectivity ratios compared to the pos. control osimertinib (A549 IC50 = 2.91 μM, H1975 IC50 = 0.064 μM). In vitro inhibitory activities against EGFR kinases containing different mutations were also tested. Compound 17i showed remarkable inhibitory activity (with IC50 value of 1.7 nM) to EGFRL858R/T790M kinase and selectivity (22-folds compared to EGFRWT kinase). Furthermore, acridine orange/ethidium bromide (AO/EB) staining assay, cell apoptosis assay, cell cycle distribution assay and wound-healing assay of the compounds 9a and 17i were performed on H1975 cell line. The results showed dose-dependent activities of the induction of apoptosis, G0/G1-phase arrestation and inhibition of migration, which were similar to the pos. control osimertinib. Addnl., mol. docking analaysis was performed to seek the possible binding mode between the selected compounds (9a, 17i-17j) and EGFRL858R/T790M kinase. The results demonstrated that compound 17i is a promising candidate and worth further study. In the experimental materials used by the author, we found 2,4-Dichloropyrimidine(cas: 3934-20-1Reference of 2,4-Dichloropyrimidine)

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.Reference of 2,4-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Kharlamova, Alisa D.; Abel, Anton S.; Averin, Alexei D.; Maloshitskaya, Olga A.; Roznyatovskiy, Vitaly A.; Savelyev, Evgenii N.; Orlinson, Boris S.; Novakov, Ivan A.; Beletskaya, Irina P. published an article in 2021. The article was titled 《Mono- and diamination of 4,6-dichloropyrimidine, 2,6-dichloropyrazine and 1,3-dichloroisoquinoline with adamantane-containing amines》, and you may find the article in Molecules.Related Products of 1193-21-1 The information in the text is summarized as follows:

N-heteroaryl substituted adamantane-containing amines, e.g., I were of substantial interest for their perspective antiviral and psychotherapeutic activities. Chlorine atom at alpha-position of N-heterocycles was substituted by amino group using convenient nucleophilic substitution reactions with a series of adamantylalkylamines. The prototropic equilibrium in these compounds was studied using NMR spectroscopy. The introduction of second amino substituent in 4-amino-6-chloropyrimidine, 2-amino-chloropyrazine and 1-amino-3-chloroisoquinoline was achieved using Pd(0) catalysis. In the experiment, the researchers used 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

In 2014,Dodonova, Jelena; Tumkevicius, Sigitas published 《Access to 6-arylpyrrolo[2,3-d]pyrimidines via a palladium-catalyzed direct C-H arylation reaction》.RSC Advances published the findings.Computed Properties of C6H3Cl2N3 The information in the text is summarized as follows:

An efficient method of palladium-catalyzed direct arylation has been developed for the selective functionalization of the C6 position of 2,4-diarylpyrrolo[2,3-d]pyrimidines I [R1 = Ph, 4-MeOC6H4, 4-(9-carbazolyl)phenyl]. Under optimal conditions, reactions with various aryl bromides R2Br [R2 = Ph, 4-NCC6H4, 4-PhC6H4, 4-(9-carbazolyl)phenyl, etc.] successfully provided a wide range of 6-arylpyrrolo[2,3-d]pyrimidines II.2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Computed Properties 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. Computed Properties 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

In 1977,Heterocycles included an article by Sakamoto, Takao; Konno, Shoetsu; Yamanaka, Hiroshi. Computed Properties of C6H8N2O. The article was titled 《Syntheses of pyrimidinyl ketones》. The information in the text is summarized as follows:

Acylpyrimidines were prepared by nitrosation of alkylpyrimidines and hydrolysis of the oximes. Nitrosation of methylpyrimidines and dehydration with POCl3 gave cyanopyrimidines which underwent Grignard reaction with EtMgBr to give ethyldihydropyrimidines. Some acetylpyrimidines were also obtained by homolytic acetylation and underwent Willgerodt-Kindler reaction to give pyrimidinethioacetamides. In the experiment, the researchers used many compounds, for example, 2-Methoxy-4-methylpyrimidine(cas: 14001-60-6Computed Properties of C6H8N2O)

2-Methoxy-4-methylpyrimidine(cas: 14001-60-6) is a member of ether. When aromatic ethers are exposed to halogen in the presence or absence of a catalyst, they undergo halogenation, such as bromination.Computed Properties of C6H8N2O

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Synthesis of Indolizines via Reaction of 2-Substituted Azaarenes with Enals by an Amine-NHC Relay Catalysis》 was written by Li, Hongxian; Li, Xiangmin; Yu, Yang; Li, Jianjun; Liu, Yuan; Li, Hao; Wang, Wei. Recommanded Product: 63155-11-3 And the article was included in Organic Letters on April 21 ,2017. The article conveys some information:

A metal-free catalytic strategy for the facile synthesis of biol. relevant mol. architectures indolizines and imidazopyridines was developed. The process is promoted by amine and N-heterocyclic carbene (NHC) relay catalysis via Michael addition-[3 + 2] fusion of simple azaarenes and α,β-unsaturated aldehydes. The preparative power is demonstrated in the synthesis of anxiolytic drug saripidem via two simple 1-pot operations with overall 45% yield. The experimental process involved the reaction of Ethyl 2-(pyrimidin-2-yl)acetate(cas: 63155-11-3Recommanded Product: 63155-11-3)

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.Recommanded Product: 63155-11-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Studies on pyrimidine derivatives. IV. Synthesis of hydroxymethylpyrimidines by means of homolytic hydroxymethylation》 was published in Heterocycles in 1977. These research results belong to Sakamoto, Takao; Kanno, Kazuko; Ono, Takayasu; Yamanaka, Hiroshi. Reference of 2-Methoxy-4-methylpyrimidine The article mentions the following:

The hydroxymethylpyrimidines I (R = HOCH2, R1 = Me, Ph, MeO, R2 = Me; R = Ph, MeO, R1 = HOCH2, R2 = Me; R = Me, R1 = HOCH2, R2 = Ph, MeO) were prepared by hydroxymethylation of I (R = H or R1 = H) with the hydroxymethyl radical generated from MeOH and (NH4)2S2O8. The experimental process involved the reaction of 2-Methoxy-4-methylpyrimidine(cas: 14001-60-6Reference of 2-Methoxy-4-methylpyrimidine)

2-Methoxy-4-methylpyrimidine(cas: 14001-60-6) is a member of ether. When aromatic ethers are exposed to halogen in the presence or absence of a catalyst, they undergo halogenation, such as bromination.Reference of 2-Methoxy-4-methylpyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthetic Route of C6H3Cl2N3In 2012 ,《Synthesis of 4-aryl-, 2,4-diaryl- and 2,4,7-triarylpyrrolo[2,3-d]pyrimidines by a combination of the Suzuki cross-coupling and N-arylation reactions》 appeared in Tetrahedron. The author of the article were Dodonova, Jelena; Skardziute, Lina; Kazlauskas, Karolis; Jursenas, Saulius; Tumkevicius, Sigitas. The article conveys some information:

A simple and facile synthesis of novel 4-aryl-2-chloro-, 2,4-diaryl- and 2,4,7-triarylpyrrolo[2,3-d]pyrimidines with various aryl and heteroaryl assemblies in the heterocyclic framework by a combination of Suzuki cross-coupling and N-arylation reactions of 2,4-dichloropyrrolo[2,3-d]pyrimidine with arylboronic acids and haloarenes are described. The majority of the synthesized compounds emit in a near UV-blue spectral range with fluorescence quantum yields up to 67%. The effect of aryl groups attached to the pyrrole ring of pyrrolopyrimidine derivatives on optical properties is discussed.2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Synthetic Route 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. Synthetic Route 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

In 2016,Galeta, Juraj; Sala, Michal; Dracinsky, Martin; Vrabel, Milan; Havlas, Zdenek; Nencka, Radim published 《Single-Step Formation of Pyrimido[4,5-d]pyridazines by a Pyrimidine-Tetrazine Tandem Reaction》.Organic Letters published the findings.Application In Synthesis of 2,4,6-Trichloropyrimidine The information in the text is summarized as follows:

A straightforward synthesis of pyrimido[4,5-d]pyridazines from pyrimidines and tetrazines under basic conditions is reported. Deprotonated, substituted 5-halopyrimidines readily react with variously substituted tetrazines in a highly regioselective manner via a complex reaction pathway, which was supported by DFT calculations This mechanism leads to the empirically observed regioisomers without going through the conceivable hetaryne intermediate. These results on 5-halopyrimidines led to development of the methodol. for preparation of opposite regioisomers based on 6-halopyrimidines. After reading the article, we found that the author used 2,4,6-Trichloropyrimidine(cas: 3764-01-0Application In Synthesis of 2,4,6-Trichloropyrimidine)

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 In Synthesis of 2,4,6-Trichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Bouffard, Elise; Zaro, Balyn W.; Dix, Melissa M.; Cravatt, Benjamin; Wong, Chi-Huey published their research in Tetrahedron Letters in 2021. The article was titled 《Refinement of covalent EGFR inhibitor AZD9291 to eliminate off-target activity》.Recommanded Product: 2,4-Dichloropyrimidine The article contains the following contents:

Non-small-cell lung cancer (NSCLC) is a major disease that accounts for 85% of all lung cancer cases which claimed around 1.8 billion lives worldwide in 2020. Tyrosine kinase inhibitors (TKIs) that target EGFR have been used for the treatment of NSCLC, but often develop drug resistance, and the covalent inhibitor AZD9291 (I) has been developed to tackle the problem of drug resistance mediated by the T790M EGFR mutation; however, there is a side effect of hyperglycemia that may be due to off-target activity. This study examines analogs of AZD9291 by chem. proteomics, identifying analogs that maintain T790M-EGFR engagement while showing reduced cross-reactivity with off-targets. In the experimental materials used by the author, we found 2,4-Dichloropyrimidine(cas: 3934-20-1Recommanded Product: 2,4-Dichloropyrimidine)

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.Recommanded Product: 2,4-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《Synthesis and biological evaluation of 6-phenylpurine linked hydroxamates as novel histone deacetylase inhibitors》 was written by Chen, Dizhong; Soh, Chang Kai; Goh, Wei Huang; Wang, Zilong; Wang, Haishan. Product Details of 90213-66-4 And the article was included in Bioorganic Chemistry in 2020. The article conveys some information:

A series of 6-phenylpurine based hydroxamates I (R = morpholin-4-yl, diethylaminyl, dimethylaminyl, pyrrolidin-1-yl; R1 = Et, iso-Pr, Pr, cyclopentyl, pentan-3-yl; R2 = 3-[(hydroxycarbamoyl)methyl]oxidanyl, 4-[4-(hydroxycarbamoyl)butoxy]methyl, 3-[4-(hydroxycarbamoyl)piperidin-1-yl]methyl, etc.) have been designed, synthesized and evaluated. Compound I (R = morpholin-4-yl; R1 = isopropyl; R2 = 3-[3-(hydroxycarbamoyl)propyl]oxidanyl (A)) and its analogs are potent histone deacetylase (HDAC) but weak PI3K/mTOR inhibitors. These compounds demonstrated broad anti-cancer activities against 38 cancer cell lines with leukemia, lymphoma, and the majority of liver cancer cell lines exhibiting the most sensitivity towards these compounds Compound (A) demonstrated modulation of HDAC targets in vitro in a dose-dependent manner. It has good in vitro ADME profile that translated into a greatly improved pharmacokinetic profile., the compound (A) also demonstrated modulation of HDACs in tumors in a PC-3 xenograft model. It was further evaluated in combination therapies in vitro. It exhibited additive or synergistic growth inhibition effect in HepG2 cells when combined with a number of approved drugs such as sorafenib, sunitinib, and erlotinib. Hence, compound (A) has the potential to be combined with the above to treat advanced liver cancer. As such, current data warrant further evaluation, optimization, and subsequent in vivo validation of the potential combination therapies. In the experimental materials used by the author, we found 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine(cas: 90213-66-4Product Details of 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. Product Details of 90213-66-4

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia