36635-79-7

Upstream product

• 92-91-1 biphenyl-4-acetaldehyde 
• 120-14-9 3,4-dimethoxy-benzaldehyde 
• 99-90-1 para-bromoacetophenone 
• 98-80-6 phenylboronic acid 

Downstream Products

• 1417894-77-9 3-(biphenyl-4-yl)-5-(3,4-dimethoxyphenyl)pyrazole 
• 1017240-38-8 C₂₃H₂₂N₂O₂ 

Relevant academic research and scientific papers

Synthesis of diverse novel compounds with anticipated antitumor activities starting with biphenyl chalcone

The chalcone as (E)-1-([1,1′-biphenyl]-4-yl)-3-(3,4-dimethoxyphenyl)prop-2-en-1-one (3) was reacted with various active methylene compounds via Michael addition reaction under different conditions. In one hand, chalcone 3 reacted with isatin and glycine in one pot reaction via 1,3-dipolar cycloaddition reaction. On the other hand, chalcone 3 was also reacted with different N-nucleophiles via direct addition on the carbonyl group to award cyclic and/or acyclic products. Meanwhile, the reaction of chalcone 3 with S-benzylthiuronium chloride afforded the thio-Michael addition product. Chalcone 3 and 10 novel synthesized compounds were screened against two cell lines (HepG2 and MCF-7). Among of them, thiosemicarbazone 16, oxime 14 and pyrimidine-2(1H)-thione 19 derivatives revealed an excellent activity against both cell lines (IC50 values = 6.79-12.91 μM), whereas thiosemicarbazone 16 (6.79 ± 0.5 and 7.58 ± 0.6 μM) showed the highest activity.

Synthesis of new schiff base of 1,3-oxazine and 1,3-thiazine derivatives derived from 4-phenyl substituted chalcones and evaluation of their antibacterial activity

Oxazine and thiazine heterocycles have distinctive interests due to their important class of natural and non-natural products and exhibit high biological activities in the pharmaceutical and biological fields. This work was planned to synthesize Schiff ba

Synthesis and biological evaluation of 3,5-substituted pyrazoles as possible antibacterial agents

The emergence of multi-drug resistant bacteria has increased the need for novel antibiotics to help overcome what may be considered the greatest threat to modern medicine. Here we report the synthesis of fifteen novel 3,5-diaryl-1H- pyrazoles obtained via

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.

Solvent free synthesis of different substituted pyrazoles under microwave irradiation via one pot synthesis and their biological evaluation

Pyrazoles and their derivative are widely used as pharmaceutical and agrochemical agents and consequently a large number of synthetic routes to pyrazole have been reported. Due to the property of reducing blood sugar by pyrazole, it has resulted in the sy

Synthesis and pharmacological evaluation of pyrazoline derivatives as new anti-inflammatory and analgesic agents

A series of 3-(4-biphenyl)-5-substituted phenyl-2-pyrazolines (2a-h) and 1-benzoyl-3-(4-biphenyl)-5-substituted phenyl-2-pyrazolines (3a-h) were synthesized by condensation of chalcones with hydrazine hydrate in solvent system ethanol and DMF. The newly synthesized compounds were screened for their anti-inflammatory and analgesic activity, and were compared with standard drug. Among the compounds studied, compound 2e showed more potent anti-inflammatory and analgesic activity than the standard drug, along with minimum ulcerogenic index.