Category: 3934-20-1

In 2019,Textile Research Journal included an article by Wan, Maosheng; Hua, Li; Zeng, Yiwen; Xie, Dengyu; Jiao, Peifu; Tong, Zhangfa. Application In Synthesis of 2,4-Dichloropyrimidine. The article was titled 《Synthesis of novel 4,4′-bis(2,4-pyrimidinyl)-diaminostilbene-2,2′-disulfonic acid derivatives and their whitening effect on cotton fiber as fluorescent whitening agents》. The information in the text is summarized as follows:

Some novel 4,4′-bis(2,4-pyrimidinyl)-diamino stilbene-2,2′-disulfonic acid derivatives 4a-d were designed and synthesized. Their structures were confirmed by proton NMR, elemental anal. and UV absorption spectra. All newly synthesized compounds were interrogated on their whitening effect on cotton fiber as fluorescent whitening agents. Their optical properties were evaluated by the degree of whiteness, color index, light fastness, wet rubbing fastness and dry rubbing fastness. The results indicated that compounds 4a-d showed an obvious whitening effect on cotton fiber and higher fastness than that of C186. The reflectivity of cotton fiber treated with compounds 4a-d at the critical concentration was up to 120.76%. In contrast, the reflectivity of untreated cotton fiber was only 87.23%. The UV absorption properties of compound 4d were tested under diverse pH values. The results showed that the UV absorption intensity of compound 4d decreased significantly and the absorption curve had blue shift under acidic conditions. Compound 4d was found to be the most effective mol. as a fluorescent whitening agent with a higher degree of whiteness (CIE Whiteness 135.04) compared to untreated cotton fiber (CIE Whiteness 73.02) at the critical concentration (0.1%). After reading the article, we found that the author used 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. 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-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application of 3934-20-1In 2020 ,《Design of new quinolin-2-one-pyrimidine hybrids as sphingosine kinases inhibitors》 appeared in Bioorganic Chemistry. The author of the article were Vettorazzi, Marcela; Insuasty, Daniel; Lima, Santiago; Gutierrez, Lucas; Nogueras, Manuel; Marchal, Antonio; Abonia, Rodrigo; Andujar, Sebastian; Spiegel, Sarah; Cobo, Justo; Enriz, Ricardo D.. The article conveys some information:

Sphingosine-1-phosphate is now emerging as an important player in cancer, inflammation, autoimmune, neurol. and cardiovascular disorders. Abundance evidence in animal and humans cancer models has shown that SphK1 is linked to cancer. Thus, there is a great interest in the development new SphK1 inhibitors as a potential new treatment for cancer. In a search for new SphK1 inhibitors we selected the well-known SKI-II inhibitor as the starting structure and we synthesized a new inhibitor structurally related to SKI-II with a significant but moderate inhibitory effect. In a second approach, based on our mol. modeling results, we designed new structures based on the structure of PF-543, the most potent known SphK1 inhibitor. Using this approach, we report the design, synthesis and biol. evaluation of a new series of compounds with inhibitory activity against both SphK1 and SphK2. These new inhibitors were obtained incorporating new connecting chains between their polar heads and hydrophobic tails. On the other hand, the combined techniques of mol. dynamics simulations and QTAIM calculations provided complete and detailed information about the mol. interactions that stabilize the different complexes of these new inhibitors with the active sites of the SphK1. This information will be useful in the design of new SphK inhibitors. The experimental part of the paper was very detailed, including the reaction process of 2,4-Dichloropyrimidine(cas: 3934-20-1Application 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.Application of 3934-20-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Yuan, Kai; Ji, Minghui; Xie, Shengnan; Qiu, Zhixia; Chen, Weijiao; Min, Wenjian; Xia, Fei; Zheng, Mingming; Wang, Xiao; Li, Jiaxing; Hou, Yi; Kuang, Wenbin; Wang, Liping; Gu, Wanjian; Li, Zhiyu; Yang, Peng published an article in 2022. The article was titled 《Discovery of Dual CDK6/PIM1 Inhibitors with a Novel Structure, High Potency, and Favorable Druggability for the Treatment of Acute Myeloid Leukemia》, and you may find the article in Journal of Medicinal Chemistry.Category: pyrimidines The information in the text is summarized as follows:

Nowadays, the simultaneous inhibition of two or more pathways plays an increasingly important role in cancer treatment due to the complex and diverse pathogenesis of cancer, and the combination of the cyclin-dependent kinase 6 (CDK6) inhibitor and PIM1 inhibitor was found to generate synergistic effects in acute myeloid leukemia (AML) treatment. Therefore, we discovered a novel lead 1 targeting CDK6/PIM1 via pharmacophore-based and structure-based virtual screening, synthesized five different series of new derivates, and obtained a potent and balanced dual CDK6/PIM1 inhibitor 51 (I), which showed high kinase selectivity. Meanwhile, 51 displayed an excellent safety profile and great pharmacokinetic properties. Furthermore, 51 displayed stronger potency in reducing the burden of AML than palbociclib and SMI-4a in vivo. In summary, we offered a new direction for AML treatment and provided a great lead compound for AML preclin. studies. The experimental process involved the reaction of 2,4-Dichloropyrimidine(cas: 3934-20-1Category: pyrimidines)

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.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2019,Chemie Ingenieur Technik included an article by Xie, Xiangzhong; Schenkendorf, Rene; Krewer, Ulrike. COA of Formula: C4H2Cl2N2. The article was titled 《The Effect of Correlated Kinetic Parameters on (Bio)Chemical Reaction Networks》. The information in the text is summarized as follows:

Exploiting the information provided by (bio)chem. reaction networks has proved beneficial for process anal. and design. To this end, parameter uncertainties have to be included in the anal. and design of (bio)chem. processes to ensure reliable model-based results. The goal is to investigate the impact of parameter correlations on (bio)chem. reaction networks and parameter sensitivities. An efficient sensitivity anal. concept is demonstrated with two simulation studies, and the results indicate a significant impact of the parameter correlations on the derived parameter sensitivities and the model-based results in general. The experimental part of the paper was very detailed, including the reaction process of 2,4-Dichloropyrimidine(cas: 3934-20-1COA of Formula: C4H2Cl2N2)

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.COA of Formula: C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application In Synthesis of 2,4-DichloropyrimidineIn 2019 ,《Structure-based design and synthesis of pyrimidine-4,6-diamine derivatives as Janus kinase 3 inhibitors》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Yu, Ru-Nan; Chen, Cheng-Juan; Shu, Lei; Yin, Yuan; Wang, Zhi-Jian; Zhang, Tian-Tai; Zhang, Da-Yong. The article conveys some information:

Janus kinases (JAKs) play a key role in the proliferation, apoptosis and differentiation of immune cells, and JAKs are considered as an attractive target for the treatment of inflammatory and autoimmune diseases. Here we show the design and optimization of pyrimidine-4,6-diamine derivatives as selectivity JAK3 inhibitors. Compound I, which might interact with unique cysteine (Cys909) residue in JAK3, exhibited excellent JAK3 inhibitory activity (IC50 = 2.1 nM) and high JAK kinase selectivity. In cellular assay, I showed moderate potency inhibiting IL-2-stimulated T cell proliferation. The data supports the further development of novel JAKs inhibitors. The experimental part of the paper was very detailed, including the reaction process of 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 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.Application In Synthesis of 2,4-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2019,Journal of Medicinal Chemistry included an article by Huang, Boshi; Chen, Wenmin; Zhao, Tong; Li, Zhenyu; Jiang, Xiangyi; Ginex, Tiziana; Vilchez, David; Luque, Francisco Javier; Kang, Dongwei; Gao, Ping; Zhang, Jian; Tian, Ye; Daelemans, Dirk; De Clercq, Erik; Pannecouque, Christophe; Zhan, Peng; Liu, Xinyong. Safety of 2,4-Dichloropyrimidine. The article was titled 《Exploiting the Tolerant Region I of the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) Binding Pocket: Discovery of Potent Diarylpyrimidine-Typed HIV-1 NNRTIs against Wild-Type and E138K Mutant Virus with Significantly Improved Water Solubility and Favorable Safety Profiles》. The information in the text is summarized as follows:

Diarylpyrimidine derivatives (DAPYs) exhibit robust anti-HIV-1 potency, although they have been compromised by E138K variant and severe side-effects and been suffering from poor water solubility In the present work, hydrophilic morpholine or methylsulfonyl and sulfamide-substituted piperazine/piperidines were introduced into the right wing of DAPYs targeting the solvent-exposed tolerant region I. The anti-HIV-1 activities of 11c (EC50(WT) = 0.0035 μM, EC50(E138K) = 0.0075 μM) were the same as and 2-fold better than that of the lead etravirine against the wild-type and E138K mutant HIV-1, resp., with a relative low cytotoxicity (CC50 ≥ 173 μM). Further test showed a significant improvement in the water solubility of 11c. Besides, 11c displayed no significant inhibition on main cytochrome P 450 enzymes and exhibited no acute/subacute toxicities at doses of 2000 mg·kg-1/50 mg·kg-1 in mice. Taken together, we consider that 11c is a promising lead for further structural optimization. The results came from multiple reactions, including the reaction of 2,4-Dichloropyrimidine(cas: 3934-20-1Safety 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.Safety of 2,4-Dichloropyrimidine

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

HPLC of Formula: 3934-20-1In 2021 ,《Structural modifications on indole and pyrimidine rings of osimertinib lead to high selectivity towards L858R/T790M double mutant enzyme and potent antitumor activity》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Liu, Qiao; Luo, Yanli; Li, Zerui; Chen, Chen; Fang, Lei. The article conveys some information:

Utilizing osimertinib as the lead compound, this work has explored the structural modifications on the indole and pyrimidine rings of osimertinib to generate novel osimertinib derivatives I (R = acetyl, cyclopropyl, prop-2-en-1-yl, oxetan-3-yl, etc; R1 = H, CF3). The in vitro enzymic and cellular studies showed that the derivatives I possessed high selectivity towards double mutant EGFR and potent antitumor activity. Particularly, compound I (R = cyclopropyl, R1 = H), the most active compound, exhibited excellent inhibitory activity against double mutant EGFR (IC50 = 0.18 nM) and wild-type EGFR (IC50 = 2.89 nM) as well as H1975 cells (IC50 = 1.44 nM). Western blot anal. showed that I (R = cyclopropyl, R1 = H) completely inhibited double mutant EGFR and Erk phosphorylation. In vivo test using xenograft model indicated that compound I (R = cyclopropyl, R1 = H) had better antitumor efficacy than osimertinib. More importantly, I (R = cyclopropyl, R1 = H) displayed many advantages in the pharmacokinetic study, including better oral bioavailability and metabolism character.2,4-Dichloropyrimidine(cas: 3934-20-1HPLC of Formula: 3934-20-1) was used in this study.

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.HPLC of Formula: 3934-20-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Gao, Ping; Song, Shu; Wang, Zhao; Sun, Lin; Zhang, Jian; Pannecouque, Christophe; De Clercq, Erik; Zhan, Peng; Liu, Xinyong published their research in Bioorganic & Medicinal Chemistry in 2021. The article was titled 《Design, synthesis and anti-HIV evaluation of novel 5-substituted diarylpyrimidine derivatives as potent HIV-1 NNRTIs》.Application of 3934-20-1 The article contains the following contents:

Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are widely used in combination therapies against HIV-1. As a continuation of authors’ efforts to discover and develop ”me-better” drugs of DAPYs, novel diarylpyrimidine derivatives I (R = Ph, 2-furyl, 3-pyridyl, etc.) were designed, synthesized and evaluated for their anti-HIV activities in MT-4 cells. All the compounds demonstrated strong inhibition activity against wide-type HIV-1 strain (IIIB) with EC50 values in the range of 2.5 nM ~0.93μM. Among them, compounds I (R = 4-pyridyl, 3-pyridyl) were the most potent ones which showed anti-HIV-1IIIB activity much superior than that of nevirapine, comparable to efavirenz and etravirine. What’s more, some compounds also showed low nanomole activity against some mutant strains such as K103N and E138K. The selected compound I (R = 4-pyridyl) was also evaluated for the activity against reverse transcriptase (RT), and exhibited submicromolar IC50 values indicating that this series compounds are specific RT inhibitors. Preliminary structure-activity relationships and modeling studies of these new analogs provide valuable avenues for future mol. optimization. In the experiment, the researchers used 2,4-Dichloropyrimidine(cas: 3934-20-1Application of 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.Application of 3934-20-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Chen, Xing; Yan, Yaoyao; Zhang, Zhaoyan; Zhang, Faming; Liu, Mingming; Du, Leran; Zhang, Haixia; Shen, Xiaobao; Zhao, Dahai; Shi, Jing Bo; Liu, Xinhua published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Discovery and In Vivo Anti-inflammatory Activity Evaluation of a Novel Non-peptidyl Non-covalent Cathepsin C Inhibitor》.Application of 3934-20-1 The article contains the following contents:

Cathepsin C (Cat C) participates in inflammation and immune regulation by affecting the activation of neutrophil serine proteases (NSPs). Therefore, cathepsin C is an attractive target for treatment of NSP-related inflammatory diseases. Here, the complete discovery process of the first potent “”non-peptidyl non-covalent cathepsin C inhibitor”” was described with hit finding, structure optimization, and lead discovery. Starting with hit 14, structure-based optimization and structure-activity relationship study were comprehensively carried out, and lead compound 54 was discovered as a potent drug-like cathepsin C inhibitor both in vivo and in vitro. Also, compound 54 (with cathepsin C Enz IC50 = 57.4 nM) exhibited effective anti-inflammatory activity in an animal model of chronic obstructive pulmonary disease. These results confirmed that the non-peptidyl and non-covalent derivative could be used as an effective cathepsin C inhibitor and encouraged us to continue further drug discovery on the basis of this finding. In the experiment, the researchers used many compounds, for example, 2,4-Dichloropyrimidine(cas: 3934-20-1Application of 3934-20-1)

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.Application of 3934-20-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In 2022,Pawara, Rahul; Ahmad, Iqrar; Nayak, Deepika; Belamkar, Sateesh; Surana, Sanjay; Kundu, Chanakya Nath; Patil, Chandragauda; Patel, Harun published an article in Journal of Molecular Structure. The title of the article was 《Design and synthesis of the novel, selective WZ4002 analogue as EGFR-L858R/T790M tyrosine kinase inhibitors for targeted drug therapy in non-small-cell lung cancer (NSCLC)》.Formula: C4H2Cl2N2 The author mentioned the following in the article:

To conquer the drug-resistance of first-generation EGFR (epidermal growth factor receptor) kinase inhibitors and second-generation inhibitors’ non-selective toxicities in Non-Small Cell Lung Cancer (NSCLC) patients, a series of WZ4002 derivatives I [R1 = 4-fluorophenyl, 3,4-dichlorophenyl, 4-bromophenyl, etc.; R2 = 3-CH2=CHC(O)NHC6H4, 4-MeC(O)-N(CH2)2N-C6H4, 3-ClCH2C(O)NHC6H4, etc.] were discovered as novel double mutant EGFR-L858R/T790M TK inhibitors. This objective was attained by employing structure-based drug design and traditional optimization strategies based on the WZ4002 scaffold. Among the synthesized compounds I, representative compounds I [R1 = 4-chloro-3-fluorophenyl, 4-bromophenyl; R2 = 3-CH2=CHC(O)-N(CH2)2N-C6H4] displayed significant anti-proliferative activity on the Gefitinib-resistant cell line NCI-H1975, with an IC50 value of 0.179μM and 0.173μM, resp. Also, these compounds exhibited moderate anti-proliferative activity against the A549 cell, with an IC50 of 0.550μM and 0.528μM resp., suggesting their improved selectivity over the mutant EGFR-L858R/T790M. Excitingly, both these compounds showed significant inhibition of the double mutant EGFR-L858R/T790M TK with an IC50 value of 0.0063μM and 0.0060μM, resp. The IC50 values of both the promising compounds against the HepG2 cell line were more than 1μM, indicating safety for normal cells. Covalent docking and MD simulation further confirm their irreversible binding mode with the target protein. These results demonstrate that compounds I [R1 = 4-chloro-3-fluorophenyl, 4-bromophenyl; R2 = 3-CH2=CHC(O)-N(CH2)2N-C6H4] would be promising lead compound-targeting double mutant EGFR-L858R/T790M TK. The results came from multiple reactions, including the reaction of 2,4-Dichloropyrimidine(cas: 3934-20-1Formula: 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.Formula: C4H2Cl2N2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia