Pyrimidines

Nakayama, Chikao published the artcileSynthetic nucleosides and nucleotides. XII. Synthesis and antiviral activities of several 1-β-D-arabinofuranosyl-5-alkyluracils and their 5′-monophosphates, HPLC of Formula: 19030-75-2, the main research area is arabinofuranosylalkyluracil preparation virucide; nucleoside arabinofuranosylalkyluracil; nucleotide arabinofuranosylalkyluracil; uracil arabinofuranosylalkyl.

Arabinofuranosyluracils I (R = Me, Et, Pr, Bu) were prepared by acid hydrolysis of anhydronucleosides II. II were prepared from pyrimidines III by 2 routes : (a) condensation with 1,2-di-O-acetyl-3-O-p-toluenesulfonyl-5-O-benzoyl-D-xylofuranose and treatment of the products with MeONa-MeOH; (b) condensation with 1-O-acetyl-2,3,5-tri-O-benzoyl-β-D-ribofuranose followed by debenzoylation and cyclization. Phosphorylation of I (R = Me, Et) or II (R = Me, Et) with tetrachloropyrophosphate in MeCn followed by treatment with acid gave 1-β-D-arabinofuranosyl-5-alkyluracil 5′-phosphates (IV). Antiviral activities of I, II, and IV against herpes simplex 1 and 2 are given; I (R = Me) and IV (R = Me) were significantly active against both the viruses.

Journal of Carbohydrates, Nucleosides, Nucleotides published new progress about Antiviral agents. 19030-75-2 belongs to class pyrimidines, name is 5-N-Propyluracil, and the molecular formula is C7H10N2O2, HPLC of Formula: 19030-75-2.

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

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

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

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

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

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

Miura, Takaaki published the artcileLead generation of heat shock protein 90 inhibitors by a combination of fragment-based approach, virtual screening, and structure-based drug design, Recommanded Product: 1-(2-Amino-4-methylpyrimidin-5-yl)ethanone, the main research area is HSP90 inhibitor virtual screening antitumor structure drug design cancer; anticancer CH5015765 preparation 3D Xray HSP90 complex crystal structure; aminotriazine aminopyrimidine derivative mol structure HSP90 target antitumor design.

Heat shock protein 90 (Hsp90) is a mol. chaperone which regulates maturation and stabilization of its substrate proteins, known as client proteins. Many client proteins of Hsp90 are involved in tumor progression and survival and therefore Hsp90 can be a good target for developing anticancer drugs. With the aim of efficiently identifying a new class of orally available inhibitors of the ATP binding site of this protein, we conducted fragment screening and virtual screening in parallel against Hsp90. This approach quickly identified 2-aminotriazine and 2-aminopyrimidine derivatives as specific ligands to Hsp90 with high ligand efficiency. In silico evaluation of the 3D X-ray Hsp90 complex structures of the identified hits allowed us to promptly design CH5015765, which showed high affinity for Hsp90 and antitumor activity in human cancer xenograft mouse models.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 66373-25-9 belongs to class pyrimidines, name is 1-(2-Amino-4-methylpyrimidin-5-yl)ethanone, and the molecular formula is C7H9N3O, Recommanded Product: 1-(2-Amino-4-methylpyrimidin-5-yl)ethanone.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Burger, Matthew T. published the artcileIdentification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer, Formula: C4HBr3N2, the main research area is morpholino heterocyclic pyrimidine preparation oral PI3 kinase inhibitor cancer; NVP-BKM120; PI3K/AKT3 pathway; phosphoinositide-3-kinase.

Phosphoinositide-3-kinases (PI3Ks) are important oncol. targets due to the deregulation of this signaling pathway in a wide variety of human cancers. Herein we describe the structure guided optimization of a series of 2-morpholino, 4-substituted, 6-heterocyclic pyrimidines where the pharmacokinetic properties were improved by modulating the electronics of the 6-position heterocycle, and the overall druglike properties were fine-tuned further by modification of the 4-position substituent. The resulting 2,4-bismorpholino 6-heterocyclic pyrimidines are potent class I PI3K inhibitors showing mechanism modulation in PI3K dependent cell lines and in vivo efficacy in tumor xenograft models with PI3K pathway deregulation (A2780 ovarian and U87MG glioma). These efforts culminated in the discovery of 15 (NVP-BKM120), currently in Phase II clin. trials for the treatment of cancer.

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, Formula: C4HBr3N2.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Kala, Pruthu published the artcileDesign, Synthesis, and Anticancer Activity of Substituted Styryl Incorporated Quinazoline Derivatives, Application In Synthesis of 5472-46-8, the main research area is styryl pyrimidopyrimidine preparation diastereoselective human anticancer.

A novel series of substituted aryl ethynyl incorporated quinazolines has been synthesized. The products have been tested for their preliminary anticancer activity against human cancer cell lines like MCF-7 (human breast cancer), A549 (human lung cancer), DU-145 (human prostate cancer), and MDA MB-231 (human breast cancer). All the synthesized compounds showed good to excellent activity against tested cell lines.

Russian Journal of General Chemistry published new progress about Antitumor agents. 5472-46-8 belongs to class pyrimidines, name is Ethyl 4-amino-2-methylpyrimidine-5-carboxylate, and the molecular formula is C8H11N3O2, Application In Synthesis of 5472-46-8.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia