116860-08-3Relevant academic research and scientific papers
Solvent-free synthesis of some1-acetyl pyrazoles
Thirunarayanan, Ganesamoorthy,Sekar, Krishnamoorthy Guna
, p. 599 - 605 (2013/11/06)
Some N-acetyl pyrazoles including 1-(3-(3,4-dichlorophenyl)-5-(substituted phenyl)-4,5-dihydro-1H-pyrazole-1-yl) ethanones have been synthesised by solvent free cyclization cum acetylation of chalcones like substituted styryl 3,4-dichlorophenyl
Synthesis and biological evaluation of pyrazole derivatives containing thiourea skeleton as anticancer agents
Lv, Peng-Cheng,Li, Huan-Qiu,Sun, Juan,Zhou, Yang,Zhu, Hai-Liang
experimental part, p. 4606 - 4614 (2010/08/05)
Two series of pyrazole derivatives designing for potential EGFR kinase inhibitors have been discovered. Some of them exhibited significant EGFR inhibitory activity. Compound 3-(3,4-dimethylphenyl)-5-(4-methoxyphenyl)-4,5- dihydro-1H-pyrazole-1-carbothioamide (C5) displayed the most potent EGFR inhibitory activity with IC50 of 0.07 μM, which was comparable to the positive control erlotinib. Docking simulation was performed to position compound C5 into the EGFR active site to determine the probable binding model. Antiproliferative assay results indicating that some of the pyrazole derivatives own high antiproliferative activity against MCF-7. Compound C5 showed significant antiproliferative activity against MCF-7 with IC50 of 0.08 μM. Therefore, compound C5 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent.
