“…As a cytidine analog, gemcitabine has been reported to have an inhibitory activity on the pyrimidine biosynthesis. In addition, a few inhibitors of the pyrimidine biosynthesis have shown to induce the innate immunity in a yet-to-be-determined manner and inhibit the virus infection. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

Enlace del recurso
Enlace del recurso
Enlace del recurso

“…This is the first occurrence of the molecular self-assembly of 1,2,4-triazolo[1,5-a]pyrimidine derivatives.…”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…In this study, the antinociceptive properties of 3,4-dihydro-2,6-diaryl-4-oxo-pyrimidine-5-carbonitrile derivatives 5a–i at doses of 25 and 50 mg/kg were evaluated in mice, using the abdominal constriction test. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…This work concerns the design and synthesis of novel, substituted 5-alkoxythieno[2,3-e][1,2,4]triazolo[4,3-c]pyrimidine derivatives 5a–p prepared from 3-amino-2-thiophenecarboxylic acid methyl ester. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…NH(2), OMe) at positions 2, 4, and 6 of the pyrimidine ring were prepared. The A-arm was modified in the para position (F or OMe) and linked to the central pyrimidine core with a variable spacer (CO, O, NH). …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…These interactions occur not only for PK-THPP, but also for the antagonist series based on 5,6,7,8 tetrahydropyrido[4,3-d]pyrimidine scaffold (THPP series). However, the marked difference in the potency of THPP series compounds such as 20b, 21, 22 and 23 (PK-THPP) respect to compounds such as 17b, inhibiting TASK-3 channels in the micromolar range is due to the presence of a hydrogen bond acceptor group that can establish interactions with the threonines of the selectivity filter.…”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…These findings were well in accordance with the proposed hypothesis that the recomposition of high-energy phosphates is promoted by non-purine-analog XOR inhibitors via the salvage pathway through blockade of hypoxanthine catabolism, whereas non-specific inhibitory effects of allopurinol on purine/pyrimidine enzymes impede this re-synthesis process. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…In this study, we cloned Dek33 by positional cloning and found that it encodes a pyrimidine reductase in riboflavin biosynthesis. In dek33, a single-base mutation (G to A) in the C-terminal COG3236 domain caused a premature stop codon (TGA), producing a weak mutant allele with only a truncated form of the DEK33 protein that occurred at much lower levels that the completed WT form, and with a reduced riboflavin content. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…We investigated whether a synthetic analogue of apigenin, the 2-(3,4-dimethoxyphenyl)-3-phenyl-4H-pyrido[1,2-a] pyrimidin-4-one (called DB103), interfered with the mechanisms involved in the angiogenic process induced by the inflammatory cytokine tumour necrosis factor (TNFα). …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…We performed RNA-Seq analysis to identify gene expression changes in SCLC biopsy samples to provide mechanistic insight into the potential utility of targeting pyrimidine biosynthesis to treat SCLC. We identified systematic dysregulation of pyrimidine biosynthesis, including elevated TYMS expression that likely contributes to the lack of efficacy for current TS inhibitors in SCLC. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…The asymmetric unit of the title compound, C(17)H(14)N(2)O, contains two independent mol­ecules each consisting of perimidine and phenol units. The tricyclic perimidine units contain naphthalene ring systems and non-planar C(4)N(2) rings adopting envelope conformations with the C atoms of the NCN groups hinged by 44.11 (7) and 48.50 (6)° with respect to the best planes of the other five atoms. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…In this current study, we reported the synthesis and biological evaluation of new [1,2,3]triazolo[4,5-d]pyrimidine derivatives as potent USP28 inhibitors. Especially, compound 19 potently inhibited USP28 (IC(50) = 1.10 ± 0.02 μmol/L, K(d) = 40 nmol/L), showing selectivity over USP7 and LSD1 (IC(50) > 100 μmol/L). …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…After preparation and identification this new reagent is used as an efficient and environmentally safe catalyst for the preparation of 1, 2, 4-triazoloquinazolinone and some pyrimidine derivatives. This method is accompanied with some superiorities such as, simple operation, mild and green conditions, use of low cost and non-hazardous natural material, short reaction times, easy preparation methods and simple work-up procedures. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…At the tested concentrations (5 and 10 µM), thieno[3,2-d]pyrimidin-4-amines 4a and 4c exhibited an inhibitory effect similar to MPC-6827 on human colorectal cancer cell proliferation.…”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…The title compounds, 2-(pyridin-2-yl)-1H-perimidine (C(16)H(11)N(3); 1), 1-methyl-2-(pyridin-2-yl)-1H-perimidine (C(17)H(13)N(3); 2), and 1,3-dimethyl-2-(pyridin-2-yl)-1H-perimidinium iodide (C(18)H(16)N(3) (+)·I(−); 3) were synthesized under mild conditions and their structures were determined by (1)H NMR spectroscopy and single-crystal X-ray analysis. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…This novel catalyst, which was fully characterized by XRD, FE-SEM, EDX, FT-IR, TGA, BET, and TEM exhibited outstanding catalytic activity for the preparation of a range of pharmaceutically important tetrazolo[1,5-a]pyrimidine-6-carbonitriles with good to excellent yields in short reaction time.…”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…A new pleuromutilin derivative, 14-O-[(4,6-Diamino-pyrimidine-2-yl) thioacetyl] mutilin (DPTM), has been synthesized and proved as a potent antibacterial agent using in vitro and in vivo assays. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…The data have been obtained for a series of pteridinone-, pyrimidine-, purine-, and pyrrolopyrimidine-based compounds, developed to establish a structure-activity relationship for RSK inhibition. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso

“…In this study, we report the synthesis of a novel series of pyrano[2,3-d]pyrimidine-2,4-dione analogues as potential inhibitors against PARP-1. …”
Enlace del recurso
Enlace del recurso
Enlace del recurso