89144-75-2Relevant academic research and scientific papers
One-pot synthesis of 3,5-diphenyl-1h-pyrazoles from chalcones and hydrazine under mechanochemical ball milling
Zhang, Ze,Tan, Ya-Jun,Wang, Chun-Shan,Wu, Hao-Hao
, p. 103 - 112 (2014/02/14)
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
Yang, Yu-Shun,Li, Qing-Shan,Sun, Shuai,Zhang, Yan-Bin,Wang, Xiao-Liang,Zhang, Fei,Tang, Jian-Feng,Zhu, Hai-Liang
, p. 6048 - 6058 (2012/11/07)
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.
Heterocycles. 3. Synthesis and Spectral Data of Some 2-Pyrazolines
El-Rayyes, Nizar R.,Hovakeemian, George H.,Hmoud, Hayat S.
, p. 225 - 229 (2007/10/02)
The reaction of 1,3-diaryl-2-propen-1-ones (Ia-o) with hydrazine and methyl- and phenylhydrazine produced different substituted 2-pyrazolines (III).The structures of these products were evident from their chemical and spectroscopic analysis.
Syntheses and Spectroscopic Characterisation of Some New 3,5-Bisaryl-2-pyrazoline Derivatives. II
Sayed, G. H.,Kjosen, H.
, p. 716 - 722 (2007/10/02)
Durch Kondensation von Hydrazin bzw. substituierten Hydrazinen mit Chalkonen wurden einige neue 3,5-bisarylierte-2-pyrazoline 4, 7-18 dargestellt.Bromierung des Pyrazolins 4 liefert das 4-Brompyrazol 20.Die Verbindungen wurden durch hochaufloesende Massen
