76973-46-1

Upstream product

• 123-11-5 4-methoxy-benzaldehyde 
• 98-86-2 acetophenone 
• 959-33-1 3-(4-methoxyphenyl)-1-phenylprop-2-en-1-one 
• 22252-15-9 trans-4-methoxychalcone 

Downstream Products

• 924864-03-9 2-[5-(4-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl]-1,3-thiazol-4(5H)-one 
• 1403750-43-5 (2,3-dihydrobenzo[b][1,4]dioxin-2-yl)(5-(4-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)methanone 
• 34221-26-6 trans-1-(4-methoxyphenyl)-2-phenylcyclopropane 
• 36988-80-4 1-acetyl-5-(4-methoxyphenyl)-3-phenyl-4,5-dihydro-(1H)-pyrazole 
• 380196-84-9 2-chloro-1-(5-(4-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)ethenone 
• 767300-62-9 1-(5-(4-methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)phenylethanone 
• 496845-50-2 1-propionyl-3-phenyl-5-(4-methoxyphenyl)-2-pyrazoline 
• 1621417-94-4 5-[5-(4-methoxyphenyl)-3-phenyl-4,5-dihydropyrazol-1-ylmethylene]-3-(3-acetoxyphenyl)-2-thioxothiazolidin-4-one 
• 1621417-87-5 5-[5-(4-methoxyphenyl)-3-phenyl-4,5-dihydropyrazol-1-ylmethylene]-2-thioxo-3-p-tolylthiazolidin-4-one 
• 1621417-83-1 3-furan-2-ylmethyl-5-[5-(4-methoxyphenyl)-3-phenyl-4,5-dihydropyrazol-1-ylmethylene]-2-thioxothiazolidin-4-one 
• 1621417-77-3 5-[5-(4-methoxyphenyl)-3-phenyl-4,5-dihydropyrazol-1-ylmethylene]-2-thioxothiazolidin-4-one 
• 1621418-04-9 5-({2-[5-(4-methoxyphenyl)-3-phenyl-4,5-dihydropyrazol-1-yl]-2-oxoethylamino}-methylene)-3-methyl-2-thioxothiazolidin-4-one 
• 1621418-03-8 5-({2-[5-(4-methoxyphenyl)-3-phenyl-4,5-dihydropyrazol-1-yl]-2-oxoethylamino}-methylene)-3-methyl-2-thioxothiazolidin-4-one 
• 32664-28-1 3-(4-methoxyphenyl)-5-phenyl-1H-pyrazole 

Relevant academic research and scientific papers

Reductive Ring-Opening 1,3-Difunctionalizations of Arylcyclopropanes with Sodium Metal

Sodium dispersion promotes reductive ring opening of arylcyclopropanes. The presence of a reduction-resistant electrophile, such as methoxypinacolatoborane, epoxide, oxetane, paraformaldehyde, or chlorotrimethylsilane, during the reductive ring opening event leads to the formation of 1,3-difunctionalized 1-arylalkanes by immediate trappings of the resulting two reactive carbanions. In particular, the ring-opening 1,3-diborylations of arylcyclopropanes afford 1,3-diborylalkanes with high syn selectivity.

A class of novel tubulin polymerization inhibitors exert effective anti-tumor activity via mitotic catastrophe

In current work, a class of novel 4,5-dihydro-1H-pyrazole-1-carboxylate derivatives (E01-E28) were designed, synthesized and evaluated. Among them, the most potent compound E24 exhibited comparable activity against a panel of cancer cells (GI50

Synthesis and evaluation of chalcone and its derivatives as potential anticholinergic agents

Background: Structural similarity in Chalcone and Pyrazoline brought our intention for the analysis of such compounds. This study involved the synthesis of chalcones and their pyrazoline derivatives and their screening as cholinesterase inhibitors. The newly synthesized compounds were also investigated for their antioxidant potential. Methods: Chalcones were synthesized by well-established methods of synthesis and their structural elucidation was carried out by H-NMR, 13C-NMR, Mass spectrometry and FTIR. For the determination of inhibition potency of synthesized compounds, spectrophotometric method was applied whereas, DPPH free radical scavenging method was used to check the antioxidant ability. Results: Chalcones and their pyrazoline derivatives were synthesized and characterised by 1HNMR, 13C-NMR, Mass spectrometry and FTIR. The compounds were screened for their anti-Alzheimer activity, which exhibited that compounds 1g, 1c and 1h, 1g showed strong inhibitory potency against acetylcholinesterase and butyrylcholinesterase, respectively. DPPH radical scavenging method was applied to check anti-oxidant potential of synthesized compounds and results explored that among all the synthesized compounds only compounds 1c and 1b showed strong scavenging potential. Conclusion: Chalcone and their pyrazoline derivatives were synthesized and screened for their anti-Alzheimer and antioxidant potential. The experimental results of anti-Alzheimer activity were compared with molecular docking studies, which showed that compounds 1g, 1c and 1h, 1g were active against AChE and BChE, respectively. Among the synthesized compounds 1c and 1b were found to be most potent antioxidants. These results suggest that compound 1b, 1c, 1g and 1h may further be explored for further developments.

Synthesis of N-Acyl Triazolyl-Pyrazolines via Acylation Initiated by the Hydrazone Moiety with Carboxylic Acids

An efficient synthesis of N-acyl/N-substituted acyl pyrazolines and their triazole hybrids have been accomplished via acylation of pyrazolines and pyrazoline-triazole hybrids with carboxylic acids and/or substituted carboxylic acids in the absence of activating agents/catalysts. In the present study, a mechanism envisaging the in situ generation of a new transient acylating intermediate has been proposed to explain the acylation.

SOCl2 catalyzed cyclization of chalcones: Synthesis and spectral studies of some bio-potent 1H pyrazoles

Some aryl-aryl 1H pyrazoles have been synthesised by cyclization of aryl chalcones and hydrazine hydrate in the presence of SOCl2. The yields of the pyrazoles are more than 85%. These pyrazoles are characterized by their physical con

SAR studies of differently functionalized chalcones based hydrazones and their cyclized derivatives as inhibitors of mammalian cathepsin B and cathepsin H

Cathepsins have emerged as potential drug targets for melanoma therapy and engrossed attention of researchers for development and evaluation of cysteine cathepsin inhibitors as cancer therapeutics. In this direction, we have designed, synthesized, and ass

One-pot synthesis of 3,5-diphenyl-1h-pyrazoles from chalcones and hydrazine under mechanochemical ball milling

A highly efficient and environmentally friendly method has been developed for facile synthesis of 3,5-diphenyl-1H-pyrazoles under mechanochemical ball-milling conditions. The advantages of short reaction time, high efficiency, no separation of in situ generated intermediate, using cheap sodium persulfate as the oxidant, together with very simple work-up procedure, make this one-pot and solvent-free protocol a green and powerful alternative to traditional methods for the synthesis of these kinds of compounds.

Design, modification and 3D QSAR studies of novel 2,3-dihydrobenzo[b][1,4] dioxin-containing 4,5-dihydro-1H-pyrazole derivatives as inhibitors of B-Raf kinase

Two series of novel 2,3-dihydrobenzo[b][1,4]dioxin-containing 4,5-dihydro-1H-pyrazole derivatives C1-C15 and D1-D15 have been synthesized and evaluated for their B-Raf inhibitory and anti-proliferation activities. Compound C14 ((3-(4-bromophenyl)-5-(2-fluorophenyl)-4,5-dihydro-1H-pyrazol-1-yl)(2,3- dihydrobenzo[b][1,4]dioxin-6-yl)methanone) showed the most potent biological activity against B-RafV600E (IC50 = 0.11 μM) and WM266.4 human melanoma cell line (GI50 = 0.58 μM), being comparable with the positive control Erlotinib and more potent than our previous best compound, while D10 ((2,3-dihydrobenzo[b][1,4]dioxin-2-yl)(5-(3- fluorophenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)methanone) performed the best in the D series (IC50 = 1.70 μM; GI50 = 1.45 μM). The docking simulation was performed to analyze the probable binding models and poses and the QSAR model was built for reasonable design of B-Raf inhibitors in future. The introduction of 2,3-dihydrobenzo[b][1,4]dioxin structure reinforced the combination of our compounds and the receptor, resulting in progress of bioactivity.

Synthesis and anticancer activity of isatin-based pyrazolines and thiazolidines conjugates

The synthesis and antitumor activity screening of novel isatin based conjugates with thiazolidine and pyrazoline moieties were performed. Reaction of 3,5-diaryl-4,5-dihydropyrazoles with chloroacetyl chloride yielded starting 2-chloro-1-(3,5-diaryl-4,5-di

Synthesis and antinociceptive activities of some pyrazoline derivatives

In the present study, some pyrazoline derivatives were synthesized to investigate their potential antinociceptive activities. 1-[(Benzoxazole/benzimidazole-2-yl)thioacetyl]pyrazoline derivatives were obtained by reacting 3,5-diaryl-1-(2-chloroacetyl)pyrazolines with 2-marcaptobenzoxazole/benzimidazole. The chemical structures of the compounds were elucidated by IR, 1H NMR and FAB+-MS spectral data and Elemental Analyses. All of the compounds (100 mg/kg) exhibited significant antinociceptive activities in both hot plate and acetic acid-induced writhing tests. Naloxone (5 mg/kg) pre-treatment reversed the antinociceptive activities suggesting the involvement of opioid system in the analgesic actions. None of the compounds impaired motor coordination of animals when assessed in the Rota-Rod model. These results support the previous papers reporting the opioid sensitive antinociceptive activities of various benzoxazole/benzimidazole-pyrazoline derivative compounds.