Zhe-Shan Quan
Yanbian University
Chemical synthesisBehavioural despair testMedicinal chemistryChemistryIn vivoAnticonvulsantQuinolineTriazoleAntidepressantCarbamazepineNeurotoxicityBicucullineToxicityMaximal electroshockED50PiPotencyStereochemistryAlkoxy groupPharmacology
126Publications
24H-index
1,726Citations
Publications 113
Newest
#1Hong-Yan Guo (Yanbian University)H-Index: 1
#2Zheng-Ai Chen (Yanbian University)H-Index: 1
Last. Zhe-Shan Quan (Yanbian University)H-Index: 24
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Nature products have been extensively used in the discovery and development of new drugs, as the most important source of drugs. The triazole ring is one of main pharmacophore of the nitrogen-containing heterocycles. Thus, a new class of triazole-containing natural product conjugates has been synthesised. These compounds reportedly exert anticancer, anti-inflammatory, antimicrobial, antiparasitic, antiviral, antioxidant, anti-Alzheimer, and enzyme inhibitory effects. This review summarises the r...
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#1Run-Hui Zhang (Yanbian University)
#2Hong-Yan Guo (Yanbian University)H-Index: 1
Last. Zhe-Shan Quan (Yanbian University)H-Index: 24
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Piperazine moiety is a cyclic molecule containing two nitrogen atoms in positions 1 and 4, as well as four carbon atoms. Piperazine is one of the most sought heterocyclics for the development of new drug candidates with a wide range of applications. Over 100 molecules with a broad range of bioactivities, including antitumor, antibacterial, anti-inflammatory, antioxidant, and other activities, were reviewed. This article reviewed investigations regarding piperazine groups for the modification of ...
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Last. Changhao Zhang (Yanbian University)H-Index: 5
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#1Fan-Fan Shang (Yanbian University)
#2Jing Ying Wang (Yanbian University)
Last. Zhe-Shan Quan (Yanbian University)H-Index: 24
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Abstract Four series of hypoxia-inducible factor-1 alpha (HIF-1α) functioning derivatives stemming from modifications to the C-29 carboxyl group of celastrol were designed and synthesized, and their anticancer activities were evaluated. To address the structure and activity relationship of each derivative, extensive structural changes were made. HRE luciferase reporter assay demonstrated that 12 modified compounds showed superior HIF-1α inhibitory activity. Among them, compound C6 exhibited the ...
2 CitationsSource
#1Run-Hui Zhang (Yanbian University)
#2Runhao Jin (Yanbian University)
Last. Chunmei Jin (Yanbian University)H-Index: 4
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Toxoplasma gondii infection is widespread worldwide, not only posing a serious threat to human food safety and animal husbandry, but also endangering human health. The selectivity index was employed to measure anti-T. gondii activity. Hederagenin (HE) exhibited potent anti-T. gondii activity and low cytotoxicity. For this reason, HE was selected for in vivo experiments. HE showed 64.8%±13.1% inhibition for peritoneal tachyzoites in mice, higher than spiramycin 56.8%±6.0%. Biochemical parameters ...
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#2Hao DengH-Index: 2
Last. Zhe-Shan QuanH-Index: 24
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Natural products and their derivatives are important sources for drug discovery; however, they usually have poor solubility and low activity and require structural modification. Amino acids are highly soluble in water and have a wide range of activities. The introduction of amino acids into natural products is expected to improve the performance of these products and minimize their adverse effects. Therefore, this review summarizes the application of amino acids in the structural modification of...
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#1Ming Bian (Yanbian University)
#2Dong Zhen (IMUN: Inner Mongolia University for Nationalities)
Last. Zhe-Shan Quan (Yanbian University)H-Index: 24
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Abstract With the aim of finding new anti-inflammatory drugs, a series of new Glycyrrhetinic acid derivatives (1-34) have been designed and synthesized by structural modification, and their anti-inflammatory activities in vitro have been evaluated. The anti-inflammatory activities assay demonstrated that compound 5b suppressed the expression of pro-inflammatory cytokines including IL-6, TNF-α and NO, it also suppressed the expression of iNOS and COX-2 in LPS-induced RAW264.7 cells in a dose-depe...
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#1Hong-Juan Liu (Yanbian University)
#2Xing Huang (Yanbian University)H-Index: 1
Last. Zhe-Shan Quan (Yanbian University)H-Index: 24
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In order to find new drugs with potent antiproliferative effect, a series of novel barbituric acid derivatives containing azoles at the C-5 position were designed, synthesized, and evaluated for antiproliferative activity against three human cancer cell lines (BEL-7402, MCF-7, and HCT-116) using MTT assay. Several of the synthesized compounds exhibited potent antiproliferative effects. The most promising compound was 5-((1-(4-(trifluoromethyl)phenyl)-1H-1,2,3-triazol-4-yl) methylene)pyrimidine-2...
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#1Qing-Kun Shen (Yanbian University)H-Index: 7
#2Guo-Hua Gong (IMUN: Inner Mongolia University for Nationalities)H-Index: 2
Last. Zhe-Shan Quan (Yanbian University)H-Index: 24
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AbstractTo develop novel anti-inflammatory agents, a series of 5-alkyl-4-oxo-4,5-dihydro-[1, 2, 4]triazolo[4,3-a]quinoxaline-1-carboxamide derivatives were designed, synthesised, and evaluated for ...
5 CitationsSource
#1Shiben Wang (Liaocheng University)H-Index: 4
#2Hui Liu (Liaocheng University)H-Index: 3
Last. Zhe-Shan Quan (Yanbian University)H-Index: 24
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Abstract In this study, a series of 1,3,4-oxadiazole derivatives (5a-s, 10a-s, and 16a-d) were designed and synthesized using maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) models, to test the anticonvulsant activity of the target compounds in vivo. The neurotoxicity (NT) of the target compounds was measured using the rotating rod (ROT) method. Seven compounds with potential activity were selected to test the 50% effective dose (ED50) and 50% toxic dose (TD50). Pharmacolo...
6 CitationsSource