403717-02-2

Upstream product

• 59-88-1 phenylhydrazine hydrochloride 
• 36640-42-3 3-(4-methoxyphenyl)-1-phenyl-1H-pyrazole-4-carboxaldehyde 
• 24310-46-1 4-methoxyacetophenone phenylhydrazone 
• 100-06-1 1-(4-methoxyphenyl)ethanone 
• 372107-36-3 3-(4-methoxyphenyl)-1-phenyl-1H-pyrazole-4-carboxylic acid 

Downstream Products

• 475680-46-7 3-(4-methoxy-phenyl)-1-phenyl-1H-pyrazole-4-carbonyl isothiocyanate 
• 376352-38-4 methyl 3-(4-methoxyphenyl)-1-phenyl-1H-pyrazole-4-carboxylate 

Relevant academic research and scientific papers

Discovery of N-(benzyloxy)-1,3-diphenyl-1H-pyrazole-4-carboxamide derivatives as potential antiproliferative agents by inhibiting MEK

Mitogen activated protein kinase (MAPK) signal transduction pathway has been proved to play an important role in tumorigenesis and cancer development. MEK inhibitor has been demonstrated significant clinical benefit for blocking MAPK pathway activation and possibly could block reactivation of the MAPK pathway at the time of BRAF inhibitor resistance. Twenty N-(benzyloxy)-1,3-diphenyl-1H-pyrazole-4-carboxamide derivatives have been designed and synthesized as MEK inhibitors, and their biological activities were evaluated. Among these compounds, compound 7b showed the most potent inhibitory activity with IC50of 91?nM for MEK1 and GI50value of 0.26?μM for A549 cells. The SAR analysis and docking simulation were performed to provide crucial pharmacophore clues that could be used in further structure optimization.

Synthesis, biological evaluation and molecular docking studies of pyrazole derivatives coupling with a thiourea moiety as novel CDKs inhibitors

It was discovered that a number of cyclin dependent kinase inhibitors containing the pyrazole core structure exhibited high inhibitory potency against broad-range CDKs and corresponding anti-proliferative activities. This information guided us to design and synthesize a series of 1,3-diphenyl-N- (phenylcarbamothioyl)-1H-pyrazole-4-carboxamide derivatives (5a-10d), and evaluate their biological activities as CDKs inhibitors. Among all the synthesized compounds, compound 10b inhibited CDK2 with an IC50 value of 25 nM, counteracting tumor cell proliferation of three cancer cell lines (H460, MCF-7, A549) in the micromolar range (from 0.75 μM to 4.21 μM), In addition, flow cytometry indicated that compound 10b could induce cycle G 0/G1 phase arrest in A549 cells with a dose dependent. Taken together, compound 10b could be selected for further preclinical evaluation.

4-Functionally substituted 3-heterylpyrazoles: VII. 3-Aryl(heteryl)-1-phenyl-4-pyrazolecarbonyl isothiocyanates

3-Aryl(heteryl)-1-phenyl-4-pyrazolecarbonyl isothiocyanates were synthesized by treatment of 3-aryl(heteryl)-1-phenyl-4-pyrazolecarbonyl chlorides with lead, sodium, or ammonium thiocyanate. Their reactions with amines, hydrazines, and acylhydrazines gave the corresponding thioureas and thiosemicarbazides.