Category: pyrimidines

Xu, Ming-Yuan published the artcileMetabolomic biomarkers in urine of rats following long-term low-dose exposure of cadmium and/or chlorpyrifos, COA of Formula: C5H7N3, the main research area is urine metabolomic biomarker cadmium chlorpyrifos exposure; Biomarker; Insecticide; Long-term exposure; Rat; Toxic metal; Urine.

Heavy metals and pesticides can be easily enriched in food chains and accumulated in organisms, thus pose significant threat to human health. However, their combined effects for long-term exposure at low dose has not been thoroughly investigated; especially there was no biofluid biomarker available to noninvasively diagnose the toxicosis of the combined exposure of the two chems. at their low levels. In this study, we investigated the change of urine metabolites of rats with 90-day exposure to heavy metal cadmium (Cd) and/or organophosphorus pesticide chlorpyrifos (CPF) using gas chromatog.-mass spectrometry (GC-MS)-based metabolomics approach. Our results showed that the interaction of Cd and CPF mainly displayed an antagonistic effect. We identified the panels of metabolite biomarkers in urine: benzoic acid and mannose were unique biomarkers for Cd exposure; creatinine and N-phenylacetyl glycine were unique biomarkers for CPF exposure; anthranilic acid, ribitol, and glucose were unique biomarkers for Cd plus CPF exposure. Our results suggest that 90-day exposure to Cd and/or CPF could cause a disturbance in energy and amino acid metabolism And urine metabolomics anal. can help understand the toxicity of low dose exposure to mixed environmental chems.

Ecotoxicology and Environmental Safety published new progress about Biomarkers. 22433-68-7 belongs to class pyrimidines, name is 4-Amino-5-methylpyrimidine, and the molecular formula is C5H7N3, COA of Formula: C5H7N3.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Tarazon, Estefania published the artcileCirculating Sphingosine-1-Phosphate as A Non-Invasive Biomarker of Heart Transplant Rejection, Recommanded Product: 5-Chloro-2-(methylthio)pyrimidine, the main research area is sphingosine phosphate non invasive biomarker heart transplant rejection.

Accumulating evidence has confirmed that the expression of sarcoplasmic reticulum calcium ATPase 2a (SERCA2a) is downregulated in heart failure and cardiac allograft rejection. Although many SERCA2a-related genes and proteins involved in the regulation of myocardial Ca2+ fluxes have been explored, its related metabolites remain poorly studied. Our main objective was to identify circulating SERCA2a-related metabolites altered in cardiac allograft rejection and to determine whether these could serve as non-invasive biomarkers. Sixty plasma samples from adult heart transplant were included in a metabolomic anal. Sphingosine-1 phosphate (S1P), metabolite closely related with SERCA, were increased in patients with cardiac rejection (p < 0.0001). S1P discriminated between patients with and without rejection: normal grafts vs. all rejecting grafts (AUC = 0.911, p < 0.0001), normal grafts vs. Grade 1 R (AUC = 0.819, p < 0.01), Grade 2 R (AUC = 0.911, p < 0.0001), Grade 3 R (AUC = 0.996, p < 0.0001). In addition, we found changes in key enzymes and receptors of S1P pathway analyzed on explanted hearts from heart failure patients. This preliminary study reveals that circulating S1P determination could be a novel approach to detect cardiac rejection, showing a robust capability for detection that improves gradually with the severity of rejection. These alterations could be relevant to better understand the involvement of calcium regulation on the pathophysiol. of rejection. Scientific Reports published new progress about Biomarkers. 38275-42-2 belongs to class pyrimidines, name is 5-Chloro-2-(methylthio)pyrimidine, and the molecular formula is C5H5ClN2S, Recommanded Product: 5-Chloro-2-(methylthio)pyrimidine.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Garzo, G. published the artcileGas chromatographic determination of 5-alkyluracils and 5-alkyldeoxyuridines using flash methylation and glass capillary columns, Recommanded Product: 5-N-Propyluracil, the main research area is uracil uridine derivative chromatog.

A sensitive anal. method was developed for 5-alkyl-substituted deoxyuridines and their main metabolites, the corresponding uracils in body fluids. The compound to be determined was methylated by the “”flash”” methylation technique, i.e., by injecting a mixture of the compounds and trimethylanilinium hydroxide (TMAH) into the hot injector of a gas chromatograph, followed by separation of the derivatives with a suitably deactivated glass capillary column. The optimal conditions for methylation were found by studying the effect of injector temperature, residence time, and TMAH/compound molar ratio on the yield of the reaction. The optimal residence time of the sample in the injector could be set by a “”semi-splitless”” injection method.

Journal of Chromatography published new progress about Body fluid. 19030-75-2 belongs to class pyrimidines, name is 5-N-Propyluracil, and the molecular formula is C7H10N2O2, Recommanded Product: 5-N-Propyluracil.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Budesinsky, Zdenek published the artcileOn the synthesis of 4- and 5-pyrimidinyldiphenyl-(1-imidazolyl)methanes and their antifungal activity, Formula: C8H9BrN2O2S, the main research area is pyrimidinyldiphenylmethane imidazolyl; imidazolylpyrimidinyldiphenylmethane; fungicide imidazolylpyrimidinyldiphenylmethane; Grignard reaction pyrimidinecarboxylate.

The title compounds I (R1 = Me, SMe; R2 = Cl, Br; R3 = 1-imidazolyl) and II (R3 = 1-imidazolyl) were prepared by treating the corresponding pyrimidinyldiphenylmethanols I (R1 and R2 = as above, R3 = OH) (III) and II (R3 = OH) (IV) with thionylbisimidazole prepared in situ from SOCl2 and imidazole in MeCN solution III and IV were obtained by the Grignard reaction from the appropriately substituted Et pyrimidinecarboxylates and PhMgBr but Et 4-methyl-2-methylthio-5-pyrimidinecarboxylate gave with PhMgBr Et 1,6-dihydro-4-methyl-2-methylthio-6-phenyl-5-pyrimidinecarboxylate. 5-Bromo-2-methylthiopyrimidine failed to give Grignard’s reagent with Mg but reacted with EtMgBr yielding 5-bromo-3,4-dihydro-4-ethyl-2-methylthiopyrimidine. Three I and II were tested against Saccharomyces pasterianus, Trichophyton mentagrophytes, Candida albicans, and Aspergillus niger and showed weaker antifungal activities compared with clotrimazole.

Collection of Czechoslovak Chemical Communications published new progress about Fungicides. 74840-38-3 belongs to class pyrimidines, name is Ethyl 5-bromo-2-(methylthio)pyrimidine-4-carboxylate, and the molecular formula is C8H9BrN2O2S, Formula: C8H9BrN2O2S.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Lefranc, Julien published the artcileDiscovery of BAY-985, a Highly Selective TBK1/IKKε Inhibitor, SDS of cas: 3122-84-7, the main research area is BAY985 TBK1 IKK epsilon inhibitor antitumor activity antiproliferative melanoma.

The serine/threonine kinase TBK1 (TANK-binding kinase 1) and its homolog IKKε are noncanonical members of the inhibitor of the nuclear factor κB (IκB) kinase family. These kinases play important roles in multiple cellular pathways and, in particular, in inflammation. Herein, we describe our investigations on a family of benzimidazoles and the identification of the potent and highly selective TBK1/IKKε inhibitor BAY-985. BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 and displays antiproliferative efficacy in the melanoma cell line SK-MEL-2 but showed only weak antitumor activity in the SK-MEL-2 human melanoma xenograft model.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 3122-84-7 belongs to class pyrimidines, name is 4-Chloro-6-(methoxymethyl)pyrimidine, and the molecular formula is C6H7ClN2O, SDS of cas: 3122-84-7.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Horiuchi, Takao published the artcileDiscovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of Cyclin D1-CDK4: Synthesis, biological evaluation and structure-activity relationships. Part 2, Recommanded Product: Thieno[2,3-d]pyrimidine, 4-chloro-6-(1,1-dimethylethyl)-, the main research area is cyclin dependent kinase 4 CDK4 inhibitor cancer; hydrazone derivative SAR preparation.

The design, synthesis and evaluation of novel thieno[2,3-d]pyrimidin-4-yl hydrazone analogs as cyclin-dependent kinase 4 (CDK4) inhibitor are described. Focusing on the optimization of the heteroaryl moiety at the hydrazone with substituted Ph groups, 4-[(methylamino)methyl]benzaldehyde (22)(I) and 5-isoindolinecarbaldehyde (24)(II) (6-tert-butylthieno[2,3-d]pyrimidin-4-yl)hydrazone derivatives have been identified. In this paper, the potency, selectivity profile and structure-activity relationships of our synthetic compounds are discussed.

Bioorganic & Medicinal Chemistry published new progress about Antitumor agents. 439692-55-4 belongs to class pyrimidines, name is Thieno[2,3-d]pyrimidine, 4-chloro-6-(1,1-dimethylethyl)-, and the molecular formula is C10H11ClN2S, Recommanded Product: Thieno[2,3-d]pyrimidine, 4-chloro-6-(1,1-dimethylethyl)-.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Axten, Jeffrey M. published the artcileDiscovery of 7-methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a potent and selective first-in-class inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK), COA of Formula: C7H5BrClN3, the main research area is methyltrifluoromethylphenylacetyldihydroindolylpyrrolopyrimidinamine preparation SAR PERK inhibitory antitumor.

Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states. Evidence that PERK is implicated in tumorigenesis and cancer cell survival stimulated our search for small mol. inhibitors. Through screening and lead optimization using the human PERK crystal structure, we discovered compound I (GSK2606414), an orally available, potent, and selective PERK inhibitor. Compound I inhibits PERK activation in cells and inhibits the growth of a human tumor xenograft in mice.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 1266343-30-9 belongs to class pyrimidines, name is 5-Bromo-4-chloro-7-methyl-7H-pyrrolo[2,3-d]pyrimidine, and the molecular formula is C7H5BrClN3, COA of Formula: C7H5BrClN3.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Burger, Matthew T. published the artcileSynthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase Inhibitors, Product Details of C4HBr3N2, the main research area is morpholino heterocyclic pyrimidine preparation phosphoinositide kinase inhibitor; PI3K/AKT pathway; phosphoinositide 3-kinase alpha.

Phosphoinositide-3-kinases (PI3K) are important oncol. targets due to the deregulation of this signaling pathway in a wide variety of human cancers. A series of 2-morpholino, 4-substituted, 6-(3-hydroxyphenyl) pyrimidines have been reported as potent inhibitors of PI3Ks. Herein, we describe the structure-guided optimization of these pyrimidines with a focus on replacing the phenol moiety, while maintaining potent target inhibition and improving in vivo properties. A series of 2-morpholino, 4-substituted, 6-heterocyclic pyrimidines, which potently inhibit PI3K, were discovered. Within this series a compound (I) was identified with suitable pharmacokinetic (PK) properties, which allowed for the establishment of a PI3K PK/pharmacodynamic-efficacy relationship as determined by in vivo inhibition of AKTSer473 phosphorylation and tumor growth inhibition in a mouse A2780 tumor xenograft model.

ACS Medicinal Chemistry Letters published new progress about Antitumor agents. 36847-11-7 belongs to class pyrimidines, name is 2,4,6-Tribromopyrimidine, and the molecular formula is C4HBr3N2, Product Details of C4HBr3N2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Easmon, J. published the artcileThiazolyl and benzothiazolyl hydrazones derived from α-(N)-acetylpyridines and diazines: synthesis, antiproliferative activity and CoMFA studies, SDS of cas: 67073-96-5, the main research area is thiazolyl hydrazone preparation antiproliferative cancer CoMFA; QSAR thiazolyl hydrazone antiproliferative cancer; benzothiazolyl hydrazone antiproliferative cancer CoMFA.

The synthesis of a series of thiazolyl and benzothiazolyl hydrazones derived from α-(N)-acylpyridines, -quinolines, -isoquinolines, -pyridazines, -pyrimidines, and -pyrazines is reported. The stereochem. of these compounds was determined by NMR spectroscopic methods. The antiproliferative activity of the novel compounds was quantified in tissue culture (melanoma, breast carcinoma, colon adenocarcinoma, epitheloid cervix carcinoma, Burkitt’s lymphoma, leukemia, and hydroxyurea sensitive and resistant myelogenous leukemia sublines). All compounds exhibited profound antiproliferative activity, in particular against Burkitt’s lymphoma cells. Out of this series, some were 13-900 times more potent than hydroxyurea and no cross-resistance to hydroxyurea was observed A predictive 3D-QSAR model using the CoMFA approach was established.

European Journal of Medicinal Chemistry published new progress about Antitumor agents. 67073-96-5 belongs to class pyrimidines, name is 1-(6-Methylpyrimidin-4-yl)ethanone, and the molecular formula is C7H8N2O, SDS of cas: 67073-96-5.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Muraoka, Masako published the artcileAlkylated pyrimidine derivatives as antiviral agents. I. Syntheses and antiviral screening of alkylpyrimidine and 5-alkyluracil nucleoside, Recommanded Product: 5-N-Propyluracil, the main research area is glucopyranosyl uracils antiviral; antiviral glucopyranosyl uracils; uracils glucopyranosyl antiviral; ribofuranosyl uracils antiviral.

5-Al-kyluracil, 3-alkyluracil, 5-alkylisocytosine, 5-alkyl-6-methylisocytosine, 3-alkyl-6-methyluracil, 1-(β-D-glucopyranosyl)-5-alkyluracil and 1-(β-D-ribofuranosyl)-5-alkyluracil were prepared and screened for antivirial activity on both RNA- and DNA-containing viruses. For RNA virus, type I Mahoney polio virus, and K-2211 strain ECHO-28 virus were used. For DNA viruses, type-I and type-12 strains adeno virus and DV 96 strain vaccinia virus were used. 5-Butyluracil and 1-(β-D-ribofuranosyl)-5-butyluracil (I) were effective against both RNA and DNA viruses. I was the more effective and exerted a broader spectrum than 5-fluorodeoxyuridine.

Chemical & Pharmaceutical Bulletin published new progress about Antiviral agents. 19030-75-2 belongs to class pyrimidines, name is 5-N-Propyluracil, and the molecular formula is C7H10N2O2, Recommanded Product: 5-N-Propyluracil.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia