28081-19-8

Upstream product

• 403-42-9 1-(4-fluorophenyl)ethanone 
• 100-10-7 4-dimethylamino-benzaldehyde 
• 63072-14-0 1-(4-fluorophenyl)-2-(triphenyl-λ⁵phosphanylidene)ethanone 
• 61011-54-9 1-(4-Fluoro-phenyl)-2-(triphenyl-λ⁵-arsanylidene)-ethanone 
• 777-15-1 4-(4-fluorophenyl)-4-oxobut-2-enoic acid 
• 28611-39-4 4-(dimethylamino)benzene-boronic acid 
• 79101-34-1 acetyl-p-fluorophenyltriphenylarsonium bromide 
• 403-29-2 2-bromo-4'-fluoroacetophenone 

Downstream Products

• 144443-01-6 {4-[5-(4-Fluoro-phenyl)-2-phenyl-2H-pyrazol-3-yl]-phenyl}-dimethyl-amine 
• 98991-41-4 {4-[2-(4-Fluoro-phenyl)-6-naphthalen-2-yl-pyridin-4-yl]-phenyl}-dimethyl-amine 
• 958456-80-9 C₁₆⁽¹¹⁾CH₁₆FNO 
• 1421637-59-3 4-dimethylamino-4'-(1-piperidyl)chalcone 

Relevant academic research and scientific papers

Discovery of heterocyclic substituted dihydropyrazoles as potent anticancer agents

In this work, a series of novel heterocyclic substituted dihydropyrazole derivatives have been prepared, and in vitro anticancer activity against a panel of human tumor cell lines by SRB were evaluated. The results indicated that piperazine substituted dihydropyrazole derivatives exhibited superior anticancer activity than that of other compounds. Especially, compounds 4g, 4h, 4l, 4m, 4o, 6g, 6j and 6l showed potent antitumor activity. Further mechanism study demonstrated that compound 4o could induce G2/M arrest in HCC1806 cell and p21 accumulation significantly.

Synthesis and biological evaluation of novel hybrid compounds between chalcone and piperazine as potential antitumor agents

Chalcones play an important role in living organisms with a wide range of biological activities including potent antitumor activity. Previously, we reported that N-aryl piperazine compounds have excellent biological activity. To further explore the struct

Conversion of iodine to fluorine-18 based on iodinated chalcone and evaluation for β-amyloid PET imaging

In the amyloid cascade hypothesis, β-amyloid (Aβ) plaques is one of the major pathological biomarkers in the Alzheimer's disease (AD) brain. We report the synthesis and evaluation of novel radiofluorinated chalcones, [18F]4-dimethylamino-4′-flu

A highly selective fluorescent chemosensor for cyanide anions based on a chalcone derivative in the presence of iron(III) ions, and its capacity for living cell imaging in mixed aqueous systems

A chalcone, 4-dimethylamino 4-fluorochalcone (1) with donor-acceptor structure characteristics is found to exhibit a distinct green fluorescence and good stability in CH3CN/water (v/v = 1: 9) buffer solution (Tris-HCl, pH = 7.4), and the in sit

Pyrazoline analogs as potential anticancer agents and their apoptosis, molecular docking, MD simulation, DNA binding and antioxidant studies

N-formyl pyrazoline derivatives (3a–3l) were designed and synthesized via Michael addition reaction through cyclization of chalcones with hydrazine hydrate in presence of formic acid. The structural elucidation of N-formyl pyrazoline derivatives was carri

Synthesis, biological activities, and docking study of novel chalcone-pleuromutilin derivatives

The issue of antibiotic resistance is becoming progressively serious these days, and the feasible solution to address it is to develop and discover novel antibiotics. The diterpene natural pleuromutilin is a prominent candidate for its special mode of act

Design, Synthesis, and Docking Study of Pyrimidine–Triazine Hybrids for GABA Estimation in Animal Epilepsy Models

A series of new pyrimidine–triazine hybrids (4a–t) was designed and synthesized, from which potent anticonvulsant agents were identified. Most of the compounds exhibited promising anticonvulsant activity against the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) tests, along with minimal motor impairment with higher safety compared to the standard drugs, phenytoin and carbamazepine. In the series, 5-(4-(4-fluorophenyl)-6-(4-hydroxyphenyl)-2-thioxo-5,6-dihydropyrimidin-1(2H)-yl)-1,2-dihydro-1,2,4-triazin-3(6H)-one (4o) and 5-(6-(4-hydroxy-3-methoxyphenyl)-4-(4-hydroxyphenyl)-2-thioxo-5,6-dihydropyrimidin-1(2H)-yl)-1,2-dihydro-1,2,4-triazin-3(6H)-one (4s) emerged as most potent anticonvulsant agents with median doses of 22.54 and 29.40 mg/kg (MES ED50), 285.02 and 293.42 mg/kg (scPTZ ED50), and 389.11 and 412.16 mg/kg (TD50), respectively. Docking studies were also performed for all synthesized compounds to get insight into the binding pattern toward the GABAA receptor as a possible mechanism of their anticonvulsant action, and in silico ADME studies were carried out to predict the safety and stability of the molecules. The increased GABA level in the experimental animals in the neurochemical estimation assay confirmed their GABAergic modulating activity. The most potent compounds were also evaluated for their neurotoxic and hepatotoxic effects. Fortunately, they did not show any sign of neurotoxicity or hepatotoxicity, suggesting that they have a broad spectrum of anticonvulsant activity with a large safety margin. Together, this research suggested that 4o and 4s may serve as leads in the discovery and development of new anticonvulsant drugs.

Concise synthesis and biological evaluation of chalcone derivatives bearing n-heterocyclic moieties

In this study, we designed and synthesized a series of chalcone derivatives bearing N-heterocyclic moieties, and screened in vitro antiinflammatory in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages and anticancer activity against a panel of hum

Synthesis, spectroscopic and computational characterization of the tautomerism of pyrazoline derivatives from chalcones

In the present study a series of novel pyrazolines derivatives has been synthesized, and their structures assigned on the basis of FT-Raman, 1H and 13C NMR spectral data and computational DFT calculations. A joint computational study using B3LYP/6-311G(2d,2p) density functional theory and FT-Raman investigation on the tautomerism of 3-(4-substituted-phenyl)-4,5-dihydro-5-(4-substituted-phenyl)pyrazole-1-carbothioamide and 3-(4-substituted-phenyl)-4,5-dihydro-5-(4-substituted-phenyl)pyrazole-1-carboxamide are presented. The structures were characterized as a minimum in the potential energy surface using DFT. The calculated Raman and NMR spectra were of such remarkable agreement to the experimental results that the equilibrium between tautomeric forms has been discussed in detail. Our study suggests the existence of tautomers, the carboxamide/carbothioamide group may tautomerize, in the solid state or in solution. Thermodynamic data calculated suggests that the R(CS)NH2 and R(CO)NH2 species are more stable than the R(CNH)SH and R(CNH)OH species. Additionally, results found for the 1H NMR shifting, pointed out to which structure is present.

Characterization of the Fluorescence Properties of 4-Dialkylaminochalcones and Investigation of the Cytotoxic Mechanism of Chalcones

Understanding the mechanisms responsible for the various biological activities of chalcones, particularly the direct cellular targets, presents an unmet challenge. Here, we prepared a series of fluorescent chalcone derivatives as chemical probes for their