3934-20-1 | Pyrimidines

Odell, Luke R.’s team published research in ChemMedChem in 2022 | CAS: 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

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)

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Han, Shuwen’s team published research in Marine Drugs in 2021 | CAS: 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.COA of Formula: C4H2Cl2N2

Han, Shuwen; Zhuang, Chunlin; Zhou, Wei; Chen, Fener published an article in 2021. The article was titled 《Structural-based optimizations of the marine-originated meridianin C as glucose uptake agents by inhibiting GSK-3β》, and you may find the article in Marine Drugs.COA of Formula: C4H2Cl2N2 The information in the text is summarized as follows:

Glycogen synthase kinase 3β (GSK-3β) is a widely investigated mol. target for numerous diseases, and inhibition of GSK-3β activity has become an attractive approach for the treatment of diabetes. Meridianin C, an indole-based natural product isolated from marine Aplidium meridianum, has been reported as a potent GSK-3β inhibitor. In the present study, applying the structural-based optimization strategy, the pyrimidine group of meridianin C was modified by introducing different substituents based on the 2-aminopyrimidines-substituted pyrazolo pyridazine scaffold. Among them, compounds B29 and B30 showed a much higher glucose uptake than meridianin C (<5%) and the pos. compound 4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione (TDZD-8, 16%), with no significant toxicity against HepG2 cells at the same time. Furthermore, they displayed good GSK-3β inhibitory activities (IC 50 = 5.85; 24.4 μM). These results suggest that these meridianin C analogs represent novel lead compounds with therapeutic potential for diabetes.2,4-Dichloropyrimidine(cas: 3934-20-1COA of Formula: C4H2Cl2N2) was used in this study.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Sun, Yiping’s team published research in Tetrahedron in 2022 | CAS: 3934-20-1

In 2022,Sun, Yiping; Qu, Hongmei; Zhang, Jiacai; Duan, Xingyu; Zhang, Xiaokun published an article in Tetrahedron. The title of the article was 《Room temperature phosphorescence, thermally activated delayed fluorescence and multicolor mechanochromic luminescence of emitters through molecular interaction and conformational modulations》.Name: 2,4-Dichloropyrimidine The author mentioned the following in the article:

Two novel heavy atom-free pure organic pyrimidine-based asym. donor-acceptor type emitters were designed and synthesized. The twisted D-A conformation was favored to produce small ΔEst and effective ISC. Excitingly, PMBT and CzPMBT showed precious fluorescence-RTP-TADF triple emission. Furthermore, PMBT responded to external stimuli of volatile solvents fumigation and different intensity grinding to generate a multicolor switching system, which included charming white light due to the dual emission of fluorescence and phosphorescence. Crystallog. anal. was conducted to explain the reasons for the differences in photophys. properties produced by the two compounds This research provides insight into the mechanism of action of RTP, TADF and multicolor MCL through intermol. interactions and conformational modulation. The experimental process involved the reaction of 2,4-Dichloropyrimidine(cas: 3934-20-1Name: 2,4-Dichloropyrimidine)

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Kruppa, Marco’s team published research in Molecules in 2022 | CAS: 3934-20-1

In 2022,Kruppa, Marco; Sommer, Gereon A.; Mueller, Thomas J. J. published an article in Molecules. The title of the article was 《Concise Syntheses of Marine (Bis)indole Alkaloids Meridianin C, D, F, and G and Scalaridine A via One-Pot Masuda Borylation-Suzuki Coupling Sequence》.Computed Properties of C4H2Cl2N2 The author mentioned the following in the article:

N-Protected 3-iodoindoles were reacted with (di)azine halides in a sequentially Pd-catalyzed one-pot fashion, i.e., by Masuda borylation-Suzuki coupling (MBSC) sequence. This methodol. was successfully applied to the concise syntheses of marine indole alkaloids meridianin C, D, F, and G, as well as to the bisindole alkaloid scalaridine A, which were obtained in moderate to excellent yield. The experimental process involved the reaction of 2,4-Dichloropyrimidine(cas: 3934-20-1Computed Properties of C4H2Cl2N2)

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Wang, Juan’s team published research in Bioorganic Chemistry in 2021 | CAS: 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.Related Products of 3934-20-1

《Molecular design and preparation of 2-aminothiazole sulfanilamide oximes as membrane active antibacterial agents for drug resistant Acinetobacter baumannii》 was written by Wang, Juan; Zhang, Peng-Li; Ansari, Mohammad Fawad; Li, Shuo; Zhou, Cheng-He. Related Products of 3934-20-1 And the article was included in Bioorganic Chemistry in 2021. The article conveys some information:

A series of 2-aminothiazole sulfanilamide oximes were developed as new membrane active antibacterial agents to conquer the microbial infection. Benzoyl derivative 10c was preponderant for the treatment of drug-resistant A. baumannii infection in contrast to norfloxacin and exerted excellent biocompatibility against mammalian cells including erythrocyte and LO2 cell line. Meanwhile, it had ability to eradicate established biofilm to alleviate the resistance burden. Mechanism investigation elucidated that compound 10c was able to disturb the membrane effectively and inhibit lactic dehydrogenase, which led to cytoplasmic content leakage. The cellular redox homeostasis was interfered via the production of reactive oxygen and nitrogen species (RONS), which further contributed to respiratory pathway inactivation and reduction of GSH activity. This work indicated that 2-aminothiazole sulfanilamide oximes could be a promising start for the exploitation of novel antibacterial agents against pathogens. In addition to this study using 2,4-Dichloropyrimidine, there are many other studies that have used 2,4-Dichloropyrimidine(cas: 3934-20-1Related Products of 3934-20-1) was used in this study.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Ding, Shi’s team published research in Bioorganic Chemistry in 2022 | CAS: 3934-20-1

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)

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Bouffard, Elise’s team published research in Tetrahedron Letters in 2021 | CAS: 3934-20-1

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)

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Darari, Mohamed’s team published research in Dalton Transactions in 2019 | CAS: 3934-20-1

The author of 《Iron(II) complexes with diazinyl-NHC ligands: impact of π-deficiency of the azine core on photophysical properties》 were Darari, Mohamed; Domenichini, Edoardo; Frances-Monerris, Antonio; Cebrian, Cristina; Magra, Kevin; Beley, Marc; Pastore, Mariachiara; Monari, Antonio; Assfeld, Xavier; Haacke, Stefan; Gros, Philippe C.. And the article was published in Dalton Transactions in 2019. Application In Synthesis of 2,4-Dichloropyrimidine The author mentioned the following in the article:

Ligand field enhancing N-heterocyclic carbene (NHC) ligands were recently shown to prevent photo-induced spin crossover in Fe(II) complexes due to their intricate effects on the electronic excited state structure. Due to their pico- to nanosecond lifetimes, these complexes are now good candidates for photo-sensitizing applications. Herein authors report the synthesis and photophys. characterization of a new family of homoleptic Fe(II) complexes with C^N^C ligands involving diazines as the central N-heteroaromatic ligand. For these four carbene bond complexes, ultrafast transient absorption spectroscopy revealed a significant improvement of the excited-state lifetime. A record 32 ps lifetime was measured for a complex bearing a ligand combining a π-deficient pyrazine nucleus and a benzimidazolylidene as NHC. When compared to other azine-based ligands investigated, they argue that the lifetimes are modulated by a small excited state barrier expressing the ability of the ligand to reach the Fe-N distance needed for internal conversion to the ground state. 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)

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Li, Xiandeng’s team published research in Bioorganic Chemistry in 2022 | CAS: 3934-20-1

Category: pyrimidinesIn 2022 ,《Synthesis and biological evaluation of 6-(pyrimidin-4-yl)-1H-pyrazolo[4,3-b]pyridine derivatives as novel dual FLT3/CDK4 inhibitors》 appeared in Bioorganic Chemistry. The author of the article were Li, Xiandeng; Yang, Tao; Hu, Mengshi; Yang, Yingxue; Tang, Minghai; Deng, Dexin; Liu, Kongjun; Fu, Suhong; Tan, Yan; Wang, Huan; Chen, Yong; Zhang, Chufeng; Guo, Yong; Peng, Bin; Si, Wenting; Yang, Zhuang; Chen, Lijuan. The article conveys some information:

Herein, based on the previously reported JAK2/FLT3 inhibitor, the synthesis, structure-activity relationship and biol. evaluation of a series of unique 6-(pyrimidin-4-yl)-1H-pyrazolo[4,3-b]pyridine derivatives, e.g., I, was described that inhibited FLT3 and CDK4 kinases. The optimized compound exhibited low nanomolar range activities with IC50 values of 11 and 7 nM for FLT3 and CDK4, resp. The experimental part of the paper was very detailed, including the reaction process of 2,4-Dichloropyrimidine(cas: 3934-20-1Category: pyrimidines)

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Wang, Xinran’s team published research in Bioorganic Chemistry in 2022 | CAS: 3934-20-1

In 2022,Wang, Xinran; Zhang, Cai; Zhang, Xiangyu; Wang, Jiming; Zhao, Liyu; Zhao, Dongmei; Cheng, Maosheng published an article in Bioorganic Chemistry. The title of the article was 《Design, synthesis and biological evaluation of 2-aminopyrimidine-based LSD1 inhibitors》.Safety of 2,4-Dichloropyrimidine The author mentioned the following in the article:

AZD9291, with excellent pharmaceutical properties, has been reported to have certain LSD1 inhibitory activity. Therefore, we carried out structural optimization based on the AZD9291 skeleton to increase the LSD1 inhibitory potential of the compound Then, a series of 2-aminopyrimidine derivatives were designed and synthesized as LSD1 inhibitors, and their structure-activity relationships were studied. The most promising compound, X43, with an IC50 of 0.89 μM showed remarkable LSD1 selectivity not only to EGFRwt (>100-fold) but also to MAO-A/B (>50-fold). Further studies showed that X43 inhibited LSD1 activity and induced the apoptosis of A549 cells in a dose-dependent manner. Meanwhile, compound X43 showed a superior ability to inhibit the proliferation of A549 and THP-1 cells, with IC50 values of 1.62 μM and 1.21 μM, resp. Then, analyses of the stability of human liver microsomes, CYP inhibition and in vivo pharmacokinetics in rats showed that X43 had favorable profiles in vitro and in vivo and the potential for further study. Our findings suggested that a 2-aminopyrimidine-based LSD1 inhibitor deserves further investigation as a treatment for LSD1-overexpressing cancer.2,4-Dichloropyrimidine(cas: 3934-20-1Safety of 2,4-Dichloropyrimidine) was used in this study.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia