132434-49-2

Upstream product

• 92-52-4 biphenyl 
• 32443-38-2 1-Biphenyl-4-yl-2-(triphenyl-λ⁵-arsanylidene)-ethanone 
• 555-16-8 4-nitrobenzaldehdye 
• 99-90-1 para-bromoacetophenone 
• 98-80-6 phenylboronic acid 
• 135-73-9 2-Bromo-4'-phenylacetophenone 
• 452-58-4 2,3-Diaminopyridine 
• 73038-39-8 3-(p-nitrophenyl)-1-biphenyl-2,3-dibromopropenone 
• 92-91-1 biphenyl-4-acetaldehyde 

Downstream Products

• 861406-42-0 C₂₅H₂₂N₄O₃ 
• 1027582-72-4 3-biphenyl-4-yl-5-(4-nitro-phenyl)-cyclohex-2-enone 
• 1027064-62-5 4-biphenyl-4-yl-6-(4-nitro-phenyl)-2-oxo-cyclohex-3-enecarboxylic acid ethyl ester 

Relevant academic research and scientific papers

Synthesis and characterization of 2-pyrazoline derivatives and their in silico and in vitro studies on antimicrobial and anticancer activities

The new series of 1-(4,5-dihydro-5-phenyl-3-diphenylpyrazol-1-yl)butan-1-one derivatives were synthesized by cyclization method using biphenyl chalcone with n-butyric acid and hydrazine hydrate. The synthesized 1-(4,5-dihydro-5-phenyl-3-diphenylpyrazol-1-

Synthesis and characterization of 2-phenylpyrazoline derivatives and evaluation of their activities against antimicrobial and breast cancer cell line in vitro and in silico studies

The new series of 2-phenylpyrazoline derivatives (2a-j) were synthesized and evaluated for their antimicrobial, in silico and in vitro anticancer activity was performed by MTT assay using MDA-MB-231 (human breast adenocarcinoma) cell line. The 2-phenylpyr

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.

A halogen substituted of compounds of preparation method

The invention discloses a type 1 shown compound preparation method, comprises the following steps: (1) condensation reaction: (2) Cyclization reaction: (3) The substitution reaction: (4) Coupling reaction: (5) Reduction reaction: (6) The diazotization reaction: Wherein X is selected from F, Cl, Br, I.

Polyaniline coated on celite, a heterogeneous support for palladium: Applications in catalytic Suzuki and one-pot Suzuki-aldol reactions

Particles of celite were coated with polyaniline, characterized and used as a support for heterogenization of palladium metal ions. The prepared heterogeneous palladium catalysts were screened for Suzuki-Miyaura and one-pot Suzuki-aldol reactions with high conversions. The process of heterogenization on celite reduces the PANI consumption ten-fold when anchoring palladium ions onto the support. The recyclable catalyst was also used for the sunlight mediated Suzuki-Miyaura reaction with good conversion.

Multicomponent Cascade Synthesis of Biaryl-Based Chalcones in Pure Water and in an Aqueous Micellar Environment

The challenging multicomponent cascade synthesis of biaryl-based chalcones was carried out in pure water and in an aqueous micellar system. The first step of the protocol was a simple Pd-catalysed, ligand-free, and aerobic Suzuki–Miyaura reaction in aqueous medium. This proved to be extremely efficient for the coupling of aryl and heteroaryl bromides with different arylboronic acids. Subsequently, the resulting intermediates underwent an in-situ aldol condensation reaction to give biaryl(hetero)chalcones in good to excellent yields. When the protocol was applied to highly lipophilic or less reactive reagents, micellar catalysis was required for good results. To achieve this, we successfully used a new surfactant obtained from renewable resources that we recently designed. Furthermore, using this additive, the catalytic system can be repeatedly recycled without significant loss of activity.

SAR studies of differently functionalized 4′-phenylchalcone based compounds as inhibitors of cathepsins B, H and L

Conditions related to the elevated levels of cathepsin B [3.4.22.1], cathepsin H [3.4.22.16] and cathepsin L [3.4.22.15] in various cancerous, rheumatoid arthritis and tissue degenerative disorders motivate the design, synthesis and evaluation of compound

Synthesis and biological activity of heterocycles from chalcone

The reaction between aromatic or heteroaromatic ortho-diamines and chalcone 1a,b is a convenient and versatile method for the preparation of condensed 1,4-diazepines 2a,b and 4a,b. 2,4-Diaryl-2,3-dihydro[1,5]benzothiazepines 5a,b were obtained from the condensation of chalcone 1a,b with 2-aminothiophenol in presence of catalytic amount of acid. The reaction of 2,3-diaminopyridine with chalcone dibromides 6a,b afforded the corresponding enaminoketones 7a,b, which cyclized to 6,8-diaryl-7,8-dihydro-9H-pyrido[4,5-b][1,4]diazepine 9a,b under acid condition. All synthesized compounds were characterized using IR, 1H NMR, 13C NMR, MS and elemental analysis. The compounds were screened for their antibacterial and antifungal activities. The synthesized compounds have shown activity against all the bacterial and fungal strains.

Synthesis and antibacterial activity of some 5-(4-biphenylyl)-7-aryl[3,4-d] [1,2,3]-benzothiadiazoles

A series of 5-(4-biphenylyl)-7-aryl[3,4-d] [1,2,3]-benzothiadiazoles were synthesized, characterized by IR, NMR and elemental analysis and evaluated for in vitro antibacterial activity against some Gram-positive and Gram-negative bacteria. The antibacterial data revealed that compounds 7a-j had better activity against tested Gram-positive organisms than the reference ciprofloxacin and norfloxacin. However, the compounds were nearly inactive against Gram-negative bacteria. Compound 7c and 7d were the most active compounds against Gram-positive bacteria.

Synthesis and antibacterial activities of some 2-amino-4,6- diarylpyrimidines

A series of 2-aminopyrimidines have been prepared by the condensation of 1-(1,1′-biphenyl-4-yl)-3-arylprop-2-en-1-ones with guanidine-nitrate and characterized on the basis of analytical and spectral data. The compounds have been screened for their antibacterial activities.