Category: 5451-40-1

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Calzaferri, Francesco; Narros-Fernandez, Paloma; de Pascual, Ricardo; de Diego, Antonio M. G.; Nicke, Annette; Egea, Javier; Garcia, Antonio G.; de los Rios, Cristobal researched the compound: 2,6-Dichloropurine( cas:5451-40-1 ).COA of Formula: C5H2Cl2N4.They published the article 《Synthesis and Pharmacological Evaluation of Novel Non-nucleotide Purine Derivatives as P2X7 Antagonists for the Treatment of Neuroinflammation》 about this compound( cas:5451-40-1 ) in Journal of Medicinal Chemistry. Keywords: purine preparation antiinflammatory activity mol docking pharmacokinetic study; xanthine preparation antiinflammatory activity mol docking pharmacokinetic study. We’ll tell you more about this compound (cas:5451-40-1).

In this work, novel blood-brain barrier (BBB)-permeable derivatives, e.g., I as potential P2X7 antagonists were designed and synthesized. They comprise purine or xanthine cores linked to an aryl group through different short spacers. Compounds were tested in YO-PRO-1 uptake assays and intracellular calcium dynamics in a human P2X7-expressing HEK293 cell line, two-electrode voltage-clamp in Xenopus laevis oocytes, and in interleukin 1β release assays in mouse peritoneal macrophages. BBB permeability was assessed by parallel artificial membrane permeability assays and P-glycoprotein ATPase activity. Dichloroarylpurinylethanones featured a certain P2X7 blockade, being compound (2-(6-chloro-9H-purin-9-yl)-1-(2,4-dichlorophenyl)ethan-1-one) (I), named ITH15004, the most potent, selective, and BBB-permeable antagonist. Compound I can be considered as a first non-nucleotide purine hit for future drug optimizations.

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Computed Properties of C5H2Cl2N4. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about An efficient regioselective synthesis of N-alkylated purine-triazole analogues. Author is Pandit, Chintan; Pandya, Mayank; Jadeja, Yashwantsinh; Gohel, Jyoti; Kapadiy, Khushal.

Nitrogen rich purine adduct 6-chloro-2-hydrazinyl-9H-purine was prepared by reaction of 2,6-dichloro purine with hydrazine hydrate and converted to 4-chloro-8-(3-phenoxyphenyl)-1H,5aH,6H-[1,2,4]triazolo[3,4-b]purine by a simple cyclization process (con.HCl & methanol) on reaction with 3-phenoxy benzaldehyde. These studies gave an idea regarding replacement of chlorine out of C-2 or C-6 position. Novelty was introduced by alkyl substation at N-9 position of imidazole ring and at -NH of triazole ring and a series of 4-chloro-5a,6-dihydro-1,6-dialkylated-8-(3-phenoxyphenyl)-1H-[1,2,4]triazolo[3,4-e]purine I [R = CH3, (CH2)2CH3, CH(CH3)2, etc.] hybrids were synthesized.

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Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Green Regioselective Synthesis of (Purin-6-yl)hydrazones.COA of Formula: C5H2Cl2N4.

Some unique purine hydrazinylidene derivatives I (R1 = Me, CN, CF3; R2 = H, Me, F; R3 = OMe, OEt, pyrazin-2-yl) were synthesized by the regioselective reaction of 2,6-dichloropurine with hydrazine hydrate, followed by condensation with com. available 1,3-dicarbonyl compounds according to a green chem. approach. The regioselectivity of chlorine substitution in 2,6-dichloropurine was established by HMBC (Heteronuclear Multiple Bond Correlation) NMR technique.

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Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Research Support, Non-U.S. Gov’t, Bioorganic Chemistry called Synthesis and biological evaluation of 6-phenylpurine linked hydroxamates as novel histone deacetylase inhibitors, Author is Chen, Dizhong; Soh, Chang Kai; Goh, Wei Huang; Wang, Zilong; Wang, Haishan, which mentions a compound: 5451-40-1, SMILESS is C2=NC1=C(C(=NC(=N1)Cl)Cl)[NH]2, Molecular C5H2Cl2N4, Formula: C5H2Cl2N4.

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.

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SDS of cas: 5451-40-1. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Adamantane-Substituted Purines and Their β-Cyclodextrin Complexes: Synthesis and Biological Activity. Author is Rouchal, Michal; Rudolfova, Jana; Krystof, Vladimir; Vojackova, Veronika; Cmelik, Richard; Vicha, Robert.

Cyclin-dependent kinases (CDKs) play an important role in the cell-division cycle. Synthetic inhibitors of CDKs are based on 2,6,9-trisubstituted purines and are developed as potential anticancer drugs; however, they have low solubility in water. In this study, authors proved that the pharmaco-chem. properties of purine-based inhibitors can be improved by appropriate substitution with the adamantane moiety. Authors prepared ten new purine derivatives with adamantane skeletons that were linked at position 6 using phenylene spacers of variable geometry and polarity. Authors demonstrated that the adamantane skeleton does not compromise the biol. activity, and some of the new purines displayed even higher inhibition activity towards CDK2/cyclin E than the parental compounds These findings were supported by a docking study, which showed an adamantane scaffold inside the binding pocket participating in the complex stabilization with non-polar interactions. In addition, authors demonstrated that β-cyclodextrin (CD) increases the drug’s solubility in water, although this is at the cost of reducing the biochem. and cellular effect. Most likely, the drug concentration, which is necessary for target engagement, was decreased by competitive drug binding within the complex with β-CD.

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The chemical properties of alicyclic heterocycles are similar to those of the corresponding chain compounds. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Synthesis and photophysical properties of 2-azolyl-6-piperidinylpurines, the main research direction is azolylpiperidinylpurine preparation fluorescence MSPR.Application In Synthesis of 2,6-Dichloropurine.

A synthesis of fluorescent 2-azolyl-6-piperidinylpurines was designed. Azolyl substituent at purine C-2 atom was introduced via nucleophilic aromatic substitution or in the case of tetrazolyl and 1,2,3-triazolyl substituents via a ring formation on a preinstalled amine or azide moiety, resp. The obtained purine intermediates were functionalized at N-9 position using Mitsunobu reaction conditions and achieved amorphous compounds, which formed a thin-layer films of good quality. The push-pull systems exhibited fluorescence with emission in range of 360-400 nm and quantum yields up to 66% in CH2Cl2 solution and up to 45% in the thin-layer film.

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Electric Literature of C5H2Cl2N4. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Repurposing Mitsunobu Reactions as a Generic Approach toward Polyethylene Derivatives. Author is Zhang, Yin; Wang, Ting; Bai, Jing; You, Wei.

Broad scope of functionality and controllable degree of functionalization are intriguing goals for the development of polar-group-functionalized polyethylene materials. Herein, we propose a generic strategy of using widely available starting materials (i.e., poly(ethylene-co-vinyl acetate), EVA) and mild Mitsunobu functionalization conditions to prepare over 30 polyethylene derivatives No noble transition metal catalysts (e.g., Ru, Mo, Pd, etc.) or corrosive/explosive reagents (e.g., HBr, NaN3, C2H4, H2, etc.) are used in the synthesis, while functional groups such as azide, aldehyde, norbornene, and thiol can be easily installed, with tunable content as high as 18 mol %. Using this practical method, we successfully prepared polyethylene-derivatized membranes with excellent antimicrobial and fluorescent properties.

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Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 5451-40-1, is researched, Molecular C5H2Cl2N4, about 1,2,3-Triazoles as leaving groups in SNAr-arbuzov reactions: synthesis of C6-phosphonated purine derivatives, the main research direction is heptyl bisphenyltriazolyl purine regioselective nucleophilic aromatic substitution Arbuzov reaction; diethoxyphosphoryl heptyl triazolyl purine preparation; 2,6-bistriazolylpurines; Arbuzov reaction; nucleophilic aromatic substitution; purinylphosphonates.Formula: C5H2Cl2N4.

A new method for C-N bond transformations into C-P bonds was developed using 1,2,3-triazoles as leaving groups in SNAr-Arbuzov reactions. A series of C6-phosphonated 2-triazolylpurine derivatives I [R = methoxycarbnonyl, Bu, 2-pyridyl, etc.] was synthesized for the first time, with the isolated yields reaching up to 82% in the C-P-bond-forming event. The SNAr-Arbuzov reaction of 2,6-bistriazolylpurines follows the general regioselectivity pattern of the C6-position being more reactive towards substitution, which was unambiguously proved by X-ray anal. of I [R = phenyl].

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Name: 2,6-Dichloropurine. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Design, synthesis and biological evaluation of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent Kinase2 (CDK2) dual inhibitors against malignant cancer. Author is Yun, Fan; Cheng, Chunhui; Ullah, Sadeeq; Yuan, Qipeng.

Designe and synthesis of series of novel histone deacetylase1/2 (HDAC1/2) and cyclin-dependent kinase2 (CDK2) dual inhibitors by integrating purine-based pharmacophore into the recognition cap group of CS055. The representative compound e.g., I [R1 = 4-MeC6H4] with excellent antiproliferative activities towards five solid cancer cells, showed potent inhibitory activities against HDAC1, HDAC2 and CDK2 with IC50 values of 70.7 nM, 23.1 nM and 0.80μM, resp. Besides, compound I could effectively block the cell cycle in the G2/M phase and induce apoptosis, which might be related to increasing intracellular ROS levels. Importantly, compound I exhibited desirable pharmacokinetic (PK) properties with the i.p. bioavailability of 50.8% in ICR mice, and potent in vivo antitumor activity in the HCT116 xenograft model. Therefore, compound I could be considered as a promising lead compound for the development of multitargeting anticancer agents.

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Name: 2,6-Dichloropurine. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 2,6-Dichloropurine, is researched, Molecular C5H2Cl2N4, CAS is 5451-40-1, about Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. Author is Ma, Xiaodong; Wei, Jun; Wang, Chang; Gu, Dongyan; Hu, Yongzhou; Sheng, Rong.

A series of 24 benzothiadiazine derivatives I (R1 = Ph, 4-F-Ph, 3-CF3-Ph, etc; R2 = H, F, Cl; R3 = Me, Et; R4 = H, F, Cl), II, III (R5 = Ph, 4-F-Ph, 4-OCF3-Ph, 3-Py; R6 = H, F) with structural novelty were designed, synthesized and biol. evaluated as PI3Kδ-selective inhibitors. Structure-activity relationship (SAR) study showed that, compounds I (R1 = Ph; R2 = Cl; R3 = Et; R4 = H) and II (R2 = Cl; R3 = Me) were identified with single-digit nanomolar IC50 values against PI3Kδ and submicromolar GI50 values against human malignant B-cell line SU-DHL-6. Furthermore, chiral resolution of the key amine intermediate of these two compounds was performed to achieve corresponding enantiomers. Compounds (S)-3-(1-((9H-purin-6-yl)amino)ethyl)-8-chloro-2-phenyl-2Hbenzo[e][1,2,4]thiadiazine 1,1-dioxide(IC50: 4.6 nM) and (S)-4-amino-6-((1-(8-chloro-1,1-dioxido-2-phenyl-2H-benzo[e][1,2,4]thiadiazin-3-yl)ethyl)amino)pyrimidine-5-carbonitrile(IC50: below 0.32 nM) demonstrated comparable and superior PI3Kδ inhibitory activity, resp., to that of idelalisib. Addnl., both the compounds exerted enhanced anti-proliferative activity against the SU-DHL-6 cell line than that of idelalisib and they exhibited excellent PI3Kδ selectivity. The in vivo pharmacokinetic (PK) study revealed that (S)-3-(1-((9H-purin-6-yl)amino)ethyl)-8-chloro-2-phenyl-2Hbenzo[e][1,2,4]thiadiazine 1,1-dioxide displayed good plasma exposure and an acceptable oral bioavailability of 29.2% and can further be developed as a potential therapeutic agent for battling B-cell-mediated malignancies.

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