Category: 3934-20-1

Barbosa da Silva, Elany; Rocha, Debora A.; Fortes, Isadora S.; Yang, Wenqian; Monti, Ludovica; Siqueira-Neto, Jair L.; Caffrey, Conor R.; McKerrow, James; Andrade, Saulo F.; Ferreira, Rafaela S. published an article in 2021. The article was titled 《Structure-Based Optimization of Quinazolines as Cruzain and TbrCATL Inhibitors》, and you may find the article in Journal of Medicinal Chemistry.Reference of 2,4-Dichloropyrimidine The information in the text is summarized as follows:

The cysteine proteases, cruzain and TbrCATL (rhodesain), are therapeutic targets for Chagas disease and Human African Trypanosomiasis, resp. Among the known inhibitors for these proteases, N4-benzyl-N2-phenylquinazoline-2,4-diamine (1a I [R1 = phenyl; R2 = benzyl] in this study), as a competitive cruzain inhibitor (Ki = 1.4μM) was described. The synthesis and biol. evaluation of 22 analogs I [R1 = Ph, 4-OH-Ph, 2-pyridyl; R2 = benzyl, Ph, 3-Cl-Ph, etc] of I [R1 = phenyl; R2 = benzyl], containing modifications in the quinazoline core, and in the substituents in positions 2 and 4 of this ring was described. The analogs I demonstrate low micromolar inhibition of the target proteases and cidal activity against Trypanosoma cruzi with up to two log selectivity indexes in counterscreens with myoblasts. Fourteen compounds were active against Trypanosoma brucei at low to mid micromolar concentrations During the optimization of I [R1 = phenyl; R2 = benzyl], structure-based design and prediction of physicochem. properties were employed to maintain potency against the enzymes while removing colloidal aggregator characteristics observed for some mols. in this series.2,4-Dichloropyrimidine(cas: 3934-20-1Reference of 2,4-Dichloropyrimidine) was used in this study.

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.Reference of 2,4-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Chen, Tianpeng; Wei, Yingying; Zhu, Gaoyang; Zhao, Huajun; Zhang, Xingxian published an article in 2021. The article was titled 《Design, synthesis and structure-activity relationship studies of 4-indole-2-arylaminopyrimidine derivatives as anti-inflammatory agents for acute lung injury》, and you may find the article in European Journal of Medicinal Chemistry.Computed Properties of C4H2Cl2N2 The information in the text is summarized as follows:

Acute lung injury/acute respiratory distress syndrome (ALI/ARDS), a clin. high mortality disease, has not been effectively treated till now, and the development of anti-acute lung injury drugs is imminent. Acute lung injury was efficiently treated by inhibiting the cascade of inflammation, and reducing the inflammatory response in the lung. A series of novel compounds with highly efficient inhibiting the expression of inflammatory factors were designed by using 4-indolyl-2-aminopyrimidine as the core skeleton. Totally eleven 4-indolyl-2-arylaminopyrimidine derivatives were designed and synthesized. As well, the related anti-ALI activity of these compounds was evaluated. Compounds I and II showed a superior activity among these compounds, and the inhibition rate of IL-6 and IL-8 release ranged from 62% to 77%, and from 65% to 72%, resp. Furthermore, most of compounds had no significant cytotoxicity in vitro. The infiltration of inflammatory cells into lung tissue significantly reduced by using compound II (20 mg/kg) in the ALI mice model, which achieved the effect of protecting lung tissue and improving ALI. In addition, the inflammatory response was inhibited by using compound II through inhibiting phosphorylation of p-38 and ERK in MAPK signaling pathway, and resulted in protective effect on ALI. These data indicated that compound II showed good anti-inflammatory activity in vitro and in vivo, which was expected to become a leading compound for the treatment of ALI. In the experiment, the researchers used many compounds, for example, 2,4-Dichloropyrimidine(cas: 3934-20-1Computed Properties 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.Computed Properties of C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Jiang, Xiangyi; Huang, Boshi; Olotu, Fisayo A.; Li, Jing; Kang, Dongwei; Wang, Zhao; De Clercq, Erik; Soliman, Mahmoud E. S.; Pannecouque, Christophe; Liu, Xinyong; Zhan, Peng published their research in European Journal of Medicinal Chemistry in 2021. The article was titled 《Exploiting the tolerant region I of the non-nucleoside reverse transcriptase inhibitor (NNRTI) binding pocket. Part 2: Discovery of diarylpyrimidine derivatives as potent HIV-1 NNRTIs with high Fsp3 values and favorable drug-like properties》.Name: 2,4-Dichloropyrimidine The article contains the following contents:

A series of novel diarylpyrimidine derivatives I [R1 = cyano, 2-cyanovinyl; R = thiomorpholino, 1-oxo-1,4-thiazinan-4-yl, 1,1-dioxo-1,4-thiazinan-4-yl, etc.] targeted the tolerant region I of the NNRTI binding pocket were designed, synthesized and biol. evaluated as potent HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) with favorable drug-like properties was studied. The most active inhibitor I [R1 = 2-cyanovinyl; R = 1,1-dioxo-1,4-thiazinan-4-yl] exhibited outstanding antiviral activity against most of the viral panel, being about 2-fold (wild-type, EC50 = 0.0021μM), 1.7-fold (K103N, EC50 = 0.0019μM), and slightly more potent (E138K, EC50 = 0.0075μM) than the NNRTI drug etravirine (ETR). Addnl., I [R1 = 2-cyanovinyl; R = 1,1-dioxo-1,4-thiazinan-4-yl] was endowed with relatively low cytotoxicity (CC50 = 18.52μM). More importantly, I [R1 = 2-cyanovinyl; R = 1,1-dioxo-1,4-thiazinan-4-yl] possessed improved drug-like properties compared to those of ETR with an increased F sp3 (Fraction of sp3 carbon atoms) value. Furthermore, the mol. dynamics simulation and mol. docking studies were implemented to reveal the binding mode of I [R1 = 2-cyanovinyl; R = 1,1-dioxo-1,4-thiazinan-4-yl] in the binding pocket. Taken together, I [R1 = 2-cyanovinyl; R = 1,1-dioxo-1,4-thiazinan-4-yl] was a promising lead compound that was worth further investigation. In the experimental materials used by the author, we found 2,4-Dichloropyrimidine(cas: 3934-20-1Name: 2,4-Dichloropyrimidine)

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.Name: 2,4-Dichloropyrimidine

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Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The author of 《I-8, a novel inhibitor of mutant IDH1, inhibits cancer progression in vitro and in vivo》 were Jia, Panli; Wu, Yao; Du, Hongzhi; Yang, Lijun; Zhang, Zhibo; Ma, Tianfang; Li, Sun; Yuan, Shengtao; Lu, Ligong; Zha, Xiaoming. And the article was published in European Journal of Pharmaceutical Sciences in 2019. Application In Synthesis of 2,4-Dichloropyrimidine The author mentioned the following in the article:

Isocitrate dehydrogenase 1 mutations have been discovered in an array of hematol. malignancies and solid tumors. These mutations could cause the production of high levels of 2-hydroxyglutarate, which in turn implicated in epigenetic changes and impaired cell differentiation. Here, we described the characterization of compound I-8, a novel mutant IDH1 inhibitor, both in vitro and in vivo. Compound I-8 specifically inhibited 2-HG production, reduced histone methylation levels, induced differentiation and depleted stem characteristics in engineered and endogenous IDH1 mutant cells. In addition, oral administration of I-8 also significantly suppressed 2-HG production and histone methylation with dose of 150 mg/kg. And I-8 treatment also could induce differentiation and attenuate stem characteristics in tumor tissue. Together, these studies indicated that compound I-8 has clin. potential in tumor therapies as a effective mutant IDH1 inhibitor, and provided scientific guidance for the development of mutant IDH1 inhibitor in the future. In addition to this study using 2,4-Dichloropyrimidine, there are many other studies that have used 2,4-Dichloropyrimidine(cas: 3934-20-1Application In Synthesis of 2,4-Dichloropyrimidine) was used in this study.

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.Application In Synthesis of 2,4-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The author of 《Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFRL858R/T790M inhibitors》 were Zhao, Bingbing; Xiao, Zhen; Qi, Jianguo; Luo, Rong; Lan, Zhou; Zhang, Yanzhuo; Hu, Xiaohan; Tang, Qidong; Zheng, Pengwu; Xu, Shan; Zhu, Wufu. And the article was published in European Journal of Medicinal Chemistry in 2019. Application In Synthesis of 2,4-Dichloropyrimidine The author mentioned the following in the article:

Third-generation epidermal growth factor receptor (EGFR)L858R/T790M inhibitors are still the main drugs for the treatment of advanced non-small cell lung cancer (NSCLC), and these drugs have achieved remarkable clin. efficacy. However, there are still many patients suffering from drug-resistant mutations and drug side effects caused by NSCLC. In this study, guided by the mol. simulation, we applied a structure-based drug design strategy (SBDD) and optimized the structure to obtain a series of potent and selective EGFRL858R/T790M inhibitors. The most potent compound 18e demonstrated excellent kinase inhibitory activity and selectivity for EGFRL858R/T790M double mutants and the IC50 value reached nanomolar level. The selectivity of 18e against wild-type EGFR was near to 200-fold. In addition, compound 18e also inhibited H1975 cells proliferation at G2/M phase and induced apoptosis at a concentration of 0.25 μM, which makes it more valuable for potential lung cancer research. In the part of experimental materials, we found many familiar compounds, such as 2,4-Dichloropyrimidine(cas: 3934-20-1Application In Synthesis of 2,4-Dichloropyrimidine)

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.Application In Synthesis of 2,4-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Manzoor, Shoaib; Petreni, Andrea; Raza, Kausar Md; Supuran, Claudiu T.; Hoda, Nasimul published their research in Bioorganic & Medicinal Chemistry Letters in 2021. The article was titled 《Novel triazole-sulfonamide bearing pyrimidine moieties with carbonic anhydrase inhibitory action: Design, synthesis, computational and enzyme inhibition studies》.Quality Control of 2,4-Dichloropyrimidine The article contains the following contents:

A series of new triazole-sulfonamide bearing pyrimidine derivatives I [R = H, Me; R1 = morpholino, 4-methylpiperazin-1-yl, 4-(4-methoxyphenyl)piperazin-1-yl, etc.] were designed and synthesized via click chem. All new compounds I were validated by 1HNMR, 13CNMR, HRMS and compound I [R = H, R1 = 1-piperidyl] was further structurally validated by X-Ray single diffraction study. These compounds I were tested as inhibitors of human carbonic anhydrase (hCA) isoforms, such as hCA I, II, IX and XII, using a stopped flow CO2 hydrase assay. Most of the compounds exhibited significant inhibitory activity against hCA II and weak inhibitory activity against hCA I. The target compounds also displayed moderate to excellent inhibitory activity against tumor-related hCAs IX and XII. Some compounds, e.g., I [R = Me, R1 = 4-(4-methoxyphenyl)piperazin-1-yl, 4-ethoxycarbonylpiperazin-1-yl, 4-(2-methoxyphenyl)piperazin-1-yl] with Ki = 9.4 nM, 1.8 nM, 0.82 nM resp. exhibited excellent inhibitory activity and selectivity profile against hCAs XII over IX. Compound I [R = Me, R1 = 4-(4-chlorobenzyl)piperazin-1-yl] displayed promising inhibitory activity and selectivity profile against both tumor-related hCAs IX (Ki = 2.9 nM) as well as XII (Ki = 0.82 nM) over hCA I and II. To understand the mol. interactions, mol. docking study of compounds I [R = Me, R1 = 4-methoxyphenyl, 4-(4-chlorobenzyl)piperazin-1-yl, 4-ethoxycarbonylpiperazin-1-yl, 4-(2-methoxyphenyl)piperazin-1-yl] with hCA XII and I [R = Me, R1 = 4-(4-chlorobenzyl)piperazin-1-yl] also with hCA IX were performed. The computational study evidenced favorable interaction between the inhibitors and active residues of both proteins. Some of these derivatives are promising leads for the development of selective, anticancer agents based on CA inhibitors. In the part of experimental materials, we found many familiar compounds, such as 2,4-Dichloropyrimidine(cas: 3934-20-1Quality Control 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.Quality Control of 2,4-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The author of 《Pd/PTABS: Low-Temperature Thioetherification of Chloro(hetero)arenes》 were Bandaru, Siva Sankar Murthy; Bhilare, Shatrughn; Cardozo, Jesvita; Chrysochos, Nicolas; Schulzke, Carola; Sanghvi, Yogesh S.; Gunturu, Krishna Chaitanya; Kapdi, Anant R.. And the article was published in Journal of Organic Chemistry in 2019. Category: pyrimidines The author mentioned the following in the article:

Heteroaryl aryl and alkyl thioethers were prepared by thioetherification reactions of aryl chlorides with aryl and alkyl thiols in the presence of Pd(OAc)2 and a phosphatriazaadamantanebutanesulfonate ligand using K3PO4 as the base in DMF at 50°. Using this method, Imuran (azathioprine) was prepared The electrostatic potentials and at. charges of phosphine ligands were calculated to understand their effect on the palladium-catalyzed thioetherification reactions. In the experiment, the researchers used many compounds, for example, 2,4-Dichloropyrimidine(cas: 3934-20-1Category: pyrimidines)

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.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Computed Properties of C4H2Cl2N2In 2020 ,《Optimization of a series of potent, selective and orally bioavailable SYK inhibitors》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Grimster, Neil P.; Gingipalli, Lakshmaiah; Barlaam, Bernard; Su, Qibin; Zheng, XiaoLan; Watson, David; Wang, Haixia; Simpson, Iain; Pike, Andy; Balazs, Amber; Boiko, Scott; Ikeda, Timothy P.; Impastato, Anna C.; Jones, Natalie H.; Kawatkar, Sameer; Kemmitt, Paul; Lamont, Scott; Patel, Joe; Read, Jon; Sarkar, Ujjal; Sha, Li; Tomlinson, Ronald C.; Wang, Haiyun; Wilson, David M.; Zehnder, Troy E.; Wang, Lianghe; Wang, Peng; Goldberg, Frederick W.; Shao, Wenlin; Fawell, Stephen; Dry, Hannah; Dowling, James E.; Edmondson, Scott D.. The article contains the following contents:

Spleen tyrosine kinase (SYK) is a non-receptor cytosolic kinase. Due to its pivotal role in B cell receptor and Fc-receptor signaling, inhibition of SYK has been targeted in a variety of disease areas. Herein, we report the optimization of a series of potent and selective SYK inhibitors, focusing on improving metabolic stability, pharmacokinetics and hERG inhibition. As a result, we identified 30, which exhibited no hERG activity but unfortunately was poorly absorbed in rats and mice. We also identified a SYK chem. probe, 17, which exhibits excellent potency at SYK, and an adequate rodent PK profile to support in vivo efficacy/PD studies. 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. 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.Computed Properties of C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Reference of 2,4-DichloropyrimidineIn 2022 ,《Development of a degrader against oncogenic fusion protein FGFR3-TACC3》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Shibata, Norihito; Cho, Nobuo; Koyama, Hiroo; Naito, Mikihiko. The article conveys some information:

Fibroblast growth factor receptor 3-transforming acidic coiled-coil containing protein 3 (FGFR3-TACC3), which has been identified in many cancers such as glioblastoma and bladder cancer, is a potent oncogenic fusion protein that induces constitutive activation of FGFR signaling, resulting in uncontrolled cell proliferation. Although several tyrosine kinase inhibitors against FGFR are currently under development, resistance to such types of inhibitors in patients has become a concern. In this study, a chimeric mol. SNIPER(TACC3)-11 I was developed and found to reduce FGFR3-TACC3 levels effectively. Compound I conjugated KHS108 (a TACC3 ligand) to an LCL161 derivative II (an inhibitor of apoptosis protein [IAP] ligand) with a PEG linker (n = 2). Mechanistical anal. showed that cellular IAP1 was required for the reduction of FGFR3-TACC3 levels. Consistent with the decrease in FGFR3-TACC3 levels, compound I suppressed the growth of FGFR3-TACC3 pos. cells. Thus, compound I is a candidate therapeutic with a novel drug modality against cancers that exhibit FGFR3-TACC3-dependent proliferation and exerts pharmacol. effects distinct from FGFR3 kinase inhibitors because it lacks substructures crucial for kinase inhibition. The experimental part of the paper was very detailed, including the reaction process of 2,4-Dichloropyrimidine(cas: 3934-20-1Reference of 2,4-Dichloropyrimidine)

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.Reference of 2,4-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

《New deferiprone derivatives as multi-functional cholinesterase inhibitors: design, synthesis and in vitro evaluation》 was published in European Journal of Medicinal Chemistry in 2020. These research results belong to Bortolami, Martina; Pandolfi, Fabiana; De Vita, Daniela; Carafa, Camilla; Messore, Antonella; Di Santo, Roberto; Feroci, Marta; Costi, Roberta; Chiarotto, Isabella; Bagetta, Donatella; Alcaro, Stefano; Colone, Marisa; Stringaro, Annarita; Scipione, Luigi. Reference of 2,4-Dichloropyrimidine The article mentions the following:

A series of deferiprone derivatives has been synthesized and evaluated in vitro with the hypothesis that they can restore the cholinergic tone and attenuate the dyshomeostasis of the metals mainly involved in the pathol. These compounds were designed as dual binding site AChE inhibitors: they possess an arylalkylamine moiety connected via an alkyl chain to a 3-hydroxy-4-pyridone fragment, to allow the simultaneous interaction with catalytic active site (CAS) and peripheral anionic site (PAS) of the enzyme. Deferiprone moiety and 2-aminopyridine, 2-aminopyrimidine or 2,4-diaminopyrimidine groups have been incorporated into these compounds, in order to obtain mols. potentially able to chelate bio-metals colocalized in Aβ plaques and involved in the generation of radical species. The compounds were tested by enzymic inhibition studies towards EeAChE and eqBChE using Ellman’s method. The most potent EeAChE inhibitor is compound I, with a Ki of 788 +/- 51 nM, while the most potent eqBChE inhibitors are compounds II and III, with Ki values of 182 +/- 18 nM and 258 +/- 25 nM resp. Among the most potent cholinesterases inhibitors, few compounds were able to form complex with iron and in some cases with copper and zinc. Moreover, these compounds were characterized by low toxicity on U-87 MG Cell Line from human brain (glioblastoma astrocytoma). In the part of experimental materials, we found many familiar compounds, such as 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