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Syntheses of 1,3,4-Thia(oxa)diazole-substituted pyrazole derivatives and Their Fungicidal Activities

Chemical Research in Chinese Universities 2004年第5期20卷 543-547页

作者： WANGWen-yan ZHAOWei-guang LIZheng-ming StateKeyLaboratoryofElemento-OrganicChemistry InstituteofElemento-OrganicChemistryNankaiUniversityTianjin300071P.R.China

A series of 1,3,4-oxadiazole or 1,3,4-thiadiazole-substituted pyrazole derivatives were synthesized from 4-pyrazole formhydrazide; their biological activities were studied. The structures of all the new compounds were confirmed by means of spectroscopic methods and microanalyses. The preliminary bioassay results indicate that some compounds of them have a good fungicidal activity against Phoma asparagi and Physalospora piricola Nose.

关键词： pyrazole derivatives Sythesis Fangicidal activity

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Structural optimization and biological evaluation of 1,5-disubstituted pyrazole-3-carboxamines as potent inhibitors of human 5-lipoxygenase

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Acta Pharmaceutica Sinica B 2016年第1期6卷 32-45页

作者： Yu Zhou Jun Liu Mingyue Zheng Shuli Zheng Chunyi Jiang Xiaomei Zhou Dong Zhang Jihui Zhao Deju Ye Mingfang Zheng Hualiang Jiang Dongxiang Liu Jian Cheng Hong Liu CAS Key Laboratory of Receptor Research Shanghai Institute of Materia MedicaChinese Academy of Sciences China Pharmaceutical University Jiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-Diseases and Institute of Neuroscience Soochow University

Human 5-lipoxygenase (5-LOX) is a well-validated drug target and its inhibitors are potential drugs for treating leukotriene-related disorders. Our previous work on structural optimization of the hit compound 2 from our in-house collection identified two lead compounds, 3a and 3b, exhibiting a potent inhibitory profile against 5-LOX with IC50 values less than 1 mu mol/L in cell-based assays. Here, we further optimized these compounds to prepare a class of novel pyrazole derivatives by opening the fused ring system. Several new compounds exhibited more potent inhibitory activity than the lead compounds against 5-LOX. In particular, compound 4e not only suppressed lipopolysaccharide-induced inflammation in brain inflammatory cells and protected neurons from oxidative toxicity, but also significantly decreased infarct damage in a mouse model of cerebral ischemia. Molecular docking analysis further confirmed the consistency of our theoretical results and experimental data. In conclusion, the excellent in vitro and in vivo inhibitory activities of these compounds against 5-LOX suggested that these novel chemical structures have a promising therapeutic potential to treat leukotriene-related disorders. (C) 2016 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.

关键词： 5-Lipoxygenase 5-LOX inhibitors pyrazole derivatives Leukotrienes-related diseases In vivo Benzo-fuse heterocyle Ischemic incults Brain inflammation

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Osmium（Ⅵ） Nitrido Complex Bearing Pyrazolate Ligand as a New Potential Anticancer Agent

Osmium（Ⅵ） Nitrido Complex Bearing Pyrazolate Ligand as a ...

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第十一届全国化学生物学学术会议

作者： Wan-Qiong Huang Peng-Chao Ji Wen-Xiu Ni Department of Chemistry Shantou University Medical College

Interest in the "platinum group" metal osmium and its compounds as potential anticancer agents is growing in recent years[1]. An osmium（VI） nitrido complex Na[OsVI（N）（tpm）2]（tpm= [5-（Thien-2-yl）-1 H-pyrazol-3-yl]methanol） has been prepared and characterized. It exhibited well antiproliferation activity with the IC50 values of 5.6–11.5 μM toward six cancer cell lines. The complex arrested the G2/M cell cycle phase and activated caspase-mediated apoptosis signal pathway of HepG2. Proteomic analysis by mass spectrometry consistently suggest that treatment of HepG2 cells with Os complex decreases DNA repair capacity while increases DNA damage accumulation and DNA replication pressure, resulting in oxidative stress, which was also evidenced by up-regulation of reactive oxygen species（ROS）, reduction of mitochondrial membrane potential（MMP） and the evocation of endoplasmic reticulum（ER） stress. The anti-cancer activity of the complex was also confirmed in vivo.

关键词： osmium complex pyrazole derivatives anticancer apoptosis

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