1123744-75-1

Upstream product

• 100-06-1 1-(4-methoxyphenyl)ethanone 
• 104-87-0 4-methyl-benzaldehyde 
• 5720-07-0 4-methoxyphenylboronic acid 
• 688782-45-8 4-chloro-6-(4-methoxyphenyl)pyrimidin-2-amine 
• 5720-05-8 4-methylphenylboronic acid 
• 30925-55-4 4'-methoxy-4-methylchalcone 
• 50-01-1 guanidine hydrochloride 
• 123-11-5 4-methoxy-benzaldehyde 
• 122-00-9 para-methylacetophenone 
• 593-85-1 diguanidine carbonate 

Downstream Products

• 1377325-05-7 N-(4-(4-methylphenyl)-6-(4-methoxyphenyl)pyrimidin-2-yl)-2-(4-methylpiperazin-1-yl)acetamide 
• 912960-77-1 4-(4-methoxyphenyl)-6-(p-tolyl)pyrimidin-2-ol 
• 1226781-08-3 C₃₃H₃₆N₄O₁₀S 
• 1223546-50-6 C₂₀H₁₈ClN₃O₂ 

Relevant academic research and scientific papers

Design and synthesis of quinoline-pyrimidine inspired hybrids as potential plasmodial inhibitors

Presently, artemisinin-based combination therapy (ACT) is the first-line therapy of Plasmodium falciparum malaria. With the emergence of malaria parasites that are resistant to ACT, alternative antimalarial therapies are urgently needed. In line with this

Design, synthesis, and biological evaluation of polyphenols with 4,6-diphenylpyrimidin-2-amine derivatives for inhibition of Aurora kinase A

Background: Several 4,6-diarylpyrimidin-2-amine derivatives show anticancer properties. However, their mode of action is not fully characterized. To develop potent anticancer chemotherapeutic agents, we designed and synthesized 25 4,6-diphenylpyrimidin-2-amine derivatives containing a guanidine moiety. Methods: Clonogenic long-term survival assays were performed to screen anticancer compounds. To derive the structural conditions showing good cytotoxicities against cancer cells, quantitative structure-activity relationships (QSAR) were calculated. Biological activities were determined by flow cytometry for cell cycle analysis and by immunoblot analysis for the detection of Aurora kinase A (AURKA) activity. Because 2-(2-Amino-6-(2,4-dimethoxyphenyl)pyrimidin-4-yl) phenol (derivative 12) selectively inhibited AURKA activity from the kinome assay, in silico docking experiments were performed to elucidate the molecular binding mode between derivative 12 and AURKA. Results: The pharmacophores were derived based on the QSAR calculations. Derivative 12 inhibited AURKA activity and reduced phosphorylation of AURKA at Thr283 in HCT116 human colon cancer cells. Derivative 12 caused the accumulation of the G2/M phase of the cell cycle and triggered the cleavages of caspase-3, caspase ?7, and poly(ADP-ribose) polymerase. The binding energies of 30 apo-AURKA – derivative 12 complexes obtained from in silico docking ranged from ?16.72 to ?11.63 kcal/mol. Conclusions: Derivative 12 is an AURKA inhibitor, which reduces clonogenicity, arrests the cell cycle at the G2/M phase, and induces caspase-mediated apoptotic cell death in HCT116 human colon cancer cells. In silico docking demonstrated that derivative 12 binds to AURKA well. The structure-activity relationship calculations showed hydrophobic substituents and 1-naphthalenyl group at the R2 position increased the activity. The existence of an H-bond acceptor at C-2 of the R1 position increased the activity, too.

Influence of the C-5 substitution in polysubstituted pyrimidines on inhibition of prostaglandin E2 production

As a part of a broader structure-activity relationship study of substituted 2-aminopyrimidines, the influence of the C-5 substitution on inhibition of prostaglandin E2 (PGE2) production was studied. Thirty compounds were prepared sta

One-Pot Three-Component Synthesis of 2-Amino Pyrimidines in Aqueous PEG-400 at Ambient Temperature

Amino pyrimidines have been synthesized by a one-pot procedure under environmentally friendly reaction conditions at room temperature. The use of aqueous PEG-400 circumvents the problems associated with the toxic, hazardous organic solvents and oxidizing agents.

A facile microwave-assisted "one-Pot" synthesis of piperazino pyrimidinyl acetamides, a class of hybrid bis heterocycles and their structural elucidation using NMR spectral techniques

An array of novel piperazino pyrimidinyl acetamides, a class of hybrid bis heterocycles are synthesized in "one-pot" by microwave irradiation method catalyzed by heterogeneous NaHSO4.SiO2 catalyst in dry media and are characterized by melting point, elemental analysis, MS, FT-IR, one-dimensional NMR (1H and 13C) and two-dimensional 1H-1H COSY and 1H-13C HSQC spectral data.

Efficient and facile three-component reaction for the synthesis of 2-amine-4,6-diarylpyrimidine under solvent-free conditions

An efficient and convenient multicomponent reaction for the preparation of 2-amine-4,6-diarylpyrimidine by aromatic aldehydes, aromatic ketones, and guanidine carbonate in the presence of sodium hydroxide under solvent-free conditions is reported. The sho