The Experts below are selected from a list of 240 Experts worldwide ranked by ideXlab platform
Shangli Zhang - One of the best experts on this subject based on the ideXlab platform.
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synthesis and discovery of a novel Pyrazole Derivative as an inhibitor of apoptosis through modulating integrin β4 ros and p53 levels in vascular endothelial cells
Bioorganic & Medicinal Chemistry, 2008Co-Authors: Bao-xiang Zhao, Lu Zhang, Xingshang Zhu, Jing Zhao, Yun Zhang, Maosheng Wan, Shangli ZhangAbstract:Abstract Recently, Pyrazole Derivatives as high affinity and selective A2A adenosine receptor antagonists have been reported. But, so far, there are no reports about the inhibitory effects of multi-substituted Pyrazole Derivatives on apoptosis of vascular endothelial cells (VECs). In this study, we synthesized six Pyrazole Derivatives and characterized the structures of the compounds by IR, 1H NMR, mass spectroscopy, and element analysis. The biology assay showed that a novel Pyrazole Derivative, ethyl 3-(o-chlorophenyl)-5-methyl-1-phenyl-1H-Pyrazole-4-carboxylate (MPD) at low concentration (25 μM) increased VECs viability and inhibited VECs apoptosis induced by deprivation of serum and FGF-2. During this process, the levels of integrin β4, reactive oxygen species (ROS), and p53 were depressed obviously. The data suggested that MPD was a potential inhibitor of apoptosis associated with the signal pathway mediated by integrin β4, ROS, and p53 in VECs.
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Synthesis and discovery of a novel Pyrazole Derivative as an inhibitor of apoptosis through modulating integrin β4, ROS, and p53 levels in vascular endothelial cells
Bioorganic & medicinal chemistry, 2008Co-Authors: Bao-xiang Zhao, Lu Zhang, Xingshang Zhu, Mao‐sheng Wan, Jing Zhao, Yun Zhang, Shangli Zhang, Jun-ying MiaoAbstract:Recently, Pyrazole Derivatives as high affinity and selective A2A adenosine receptor antagonists have been reported. But, so far, there are no reports about the inhibitory effects of multi-substituted Pyrazole Derivatives on apoptosis of vascular endothelial cells (VECs). In this study, we synthesized six Pyrazole Derivatives and characterized the structures of the compounds by IR, (1)H NMR, mass spectroscopy, and element analysis. The biology assay showed that a novel Pyrazole Derivative, ethyl 3-(o-chlorophenyl)-5-methyl-1-phenyl-1H-Pyrazole-4-carboxylate (MPD) at low concentration (25muM) increased VECs viability and inhibited VECs apoptosis induced by deprivation of serum and FGF-2. During this process, the levels of integrin beta4, reactive oxygen species (ROS), and p53 were depressed obviously. The data suggested that MPD was a potential inhibitor of apoptosis associated with the signal pathway mediated by integrin beta4, ROS, and p53 in VECs.
Jing Zhao - One of the best experts on this subject based on the ideXlab platform.
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synthesis and discovery of a novel Pyrazole Derivative as an inhibitor of apoptosis through modulating integrin β4 ros and p53 levels in vascular endothelial cells
Bioorganic & Medicinal Chemistry, 2008Co-Authors: Bao-xiang Zhao, Lu Zhang, Xingshang Zhu, Jing Zhao, Yun Zhang, Maosheng Wan, Shangli ZhangAbstract:Abstract Recently, Pyrazole Derivatives as high affinity and selective A2A adenosine receptor antagonists have been reported. But, so far, there are no reports about the inhibitory effects of multi-substituted Pyrazole Derivatives on apoptosis of vascular endothelial cells (VECs). In this study, we synthesized six Pyrazole Derivatives and characterized the structures of the compounds by IR, 1H NMR, mass spectroscopy, and element analysis. The biology assay showed that a novel Pyrazole Derivative, ethyl 3-(o-chlorophenyl)-5-methyl-1-phenyl-1H-Pyrazole-4-carboxylate (MPD) at low concentration (25 μM) increased VECs viability and inhibited VECs apoptosis induced by deprivation of serum and FGF-2. During this process, the levels of integrin β4, reactive oxygen species (ROS), and p53 were depressed obviously. The data suggested that MPD was a potential inhibitor of apoptosis associated with the signal pathway mediated by integrin β4, ROS, and p53 in VECs.
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Synthesis and discovery of a novel Pyrazole Derivative as an inhibitor of apoptosis through modulating integrin β4, ROS, and p53 levels in vascular endothelial cells
Bioorganic & medicinal chemistry, 2008Co-Authors: Bao-xiang Zhao, Lu Zhang, Xingshang Zhu, Mao‐sheng Wan, Jing Zhao, Yun Zhang, Shangli Zhang, Jun-ying MiaoAbstract:Recently, Pyrazole Derivatives as high affinity and selective A2A adenosine receptor antagonists have been reported. But, so far, there are no reports about the inhibitory effects of multi-substituted Pyrazole Derivatives on apoptosis of vascular endothelial cells (VECs). In this study, we synthesized six Pyrazole Derivatives and characterized the structures of the compounds by IR, (1)H NMR, mass spectroscopy, and element analysis. The biology assay showed that a novel Pyrazole Derivative, ethyl 3-(o-chlorophenyl)-5-methyl-1-phenyl-1H-Pyrazole-4-carboxylate (MPD) at low concentration (25muM) increased VECs viability and inhibited VECs apoptosis induced by deprivation of serum and FGF-2. During this process, the levels of integrin beta4, reactive oxygen species (ROS), and p53 were depressed obviously. The data suggested that MPD was a potential inhibitor of apoptosis associated with the signal pathway mediated by integrin beta4, ROS, and p53 in VECs.
Xingshang Zhu - One of the best experts on this subject based on the ideXlab platform.
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synthesis and discovery of a novel Pyrazole Derivative as an inhibitor of apoptosis through modulating integrin β4 ros and p53 levels in vascular endothelial cells
Bioorganic & Medicinal Chemistry, 2008Co-Authors: Bao-xiang Zhao, Lu Zhang, Xingshang Zhu, Jing Zhao, Yun Zhang, Maosheng Wan, Shangli ZhangAbstract:Abstract Recently, Pyrazole Derivatives as high affinity and selective A2A adenosine receptor antagonists have been reported. But, so far, there are no reports about the inhibitory effects of multi-substituted Pyrazole Derivatives on apoptosis of vascular endothelial cells (VECs). In this study, we synthesized six Pyrazole Derivatives and characterized the structures of the compounds by IR, 1H NMR, mass spectroscopy, and element analysis. The biology assay showed that a novel Pyrazole Derivative, ethyl 3-(o-chlorophenyl)-5-methyl-1-phenyl-1H-Pyrazole-4-carboxylate (MPD) at low concentration (25 μM) increased VECs viability and inhibited VECs apoptosis induced by deprivation of serum and FGF-2. During this process, the levels of integrin β4, reactive oxygen species (ROS), and p53 were depressed obviously. The data suggested that MPD was a potential inhibitor of apoptosis associated with the signal pathway mediated by integrin β4, ROS, and p53 in VECs.
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Synthesis and discovery of a novel Pyrazole Derivative as an inhibitor of apoptosis through modulating integrin β4, ROS, and p53 levels in vascular endothelial cells
Bioorganic & medicinal chemistry, 2008Co-Authors: Bao-xiang Zhao, Lu Zhang, Xingshang Zhu, Mao‐sheng Wan, Jing Zhao, Yun Zhang, Shangli Zhang, Jun-ying MiaoAbstract:Recently, Pyrazole Derivatives as high affinity and selective A2A adenosine receptor antagonists have been reported. But, so far, there are no reports about the inhibitory effects of multi-substituted Pyrazole Derivatives on apoptosis of vascular endothelial cells (VECs). In this study, we synthesized six Pyrazole Derivatives and characterized the structures of the compounds by IR, (1)H NMR, mass spectroscopy, and element analysis. The biology assay showed that a novel Pyrazole Derivative, ethyl 3-(o-chlorophenyl)-5-methyl-1-phenyl-1H-Pyrazole-4-carboxylate (MPD) at low concentration (25muM) increased VECs viability and inhibited VECs apoptosis induced by deprivation of serum and FGF-2. During this process, the levels of integrin beta4, reactive oxygen species (ROS), and p53 were depressed obviously. The data suggested that MPD was a potential inhibitor of apoptosis associated with the signal pathway mediated by integrin beta4, ROS, and p53 in VECs.
Lu Zhang - One of the best experts on this subject based on the ideXlab platform.
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synthesis and discovery of a novel Pyrazole Derivative as an inhibitor of apoptosis through modulating integrin β4 ros and p53 levels in vascular endothelial cells
Bioorganic & Medicinal Chemistry, 2008Co-Authors: Bao-xiang Zhao, Lu Zhang, Xingshang Zhu, Jing Zhao, Yun Zhang, Maosheng Wan, Shangli ZhangAbstract:Abstract Recently, Pyrazole Derivatives as high affinity and selective A2A adenosine receptor antagonists have been reported. But, so far, there are no reports about the inhibitory effects of multi-substituted Pyrazole Derivatives on apoptosis of vascular endothelial cells (VECs). In this study, we synthesized six Pyrazole Derivatives and characterized the structures of the compounds by IR, 1H NMR, mass spectroscopy, and element analysis. The biology assay showed that a novel Pyrazole Derivative, ethyl 3-(o-chlorophenyl)-5-methyl-1-phenyl-1H-Pyrazole-4-carboxylate (MPD) at low concentration (25 μM) increased VECs viability and inhibited VECs apoptosis induced by deprivation of serum and FGF-2. During this process, the levels of integrin β4, reactive oxygen species (ROS), and p53 were depressed obviously. The data suggested that MPD was a potential inhibitor of apoptosis associated with the signal pathway mediated by integrin β4, ROS, and p53 in VECs.
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Synthesis and discovery of a novel Pyrazole Derivative as an inhibitor of apoptosis through modulating integrin β4, ROS, and p53 levels in vascular endothelial cells
Bioorganic & medicinal chemistry, 2008Co-Authors: Bao-xiang Zhao, Lu Zhang, Xingshang Zhu, Mao‐sheng Wan, Jing Zhao, Yun Zhang, Shangli Zhang, Jun-ying MiaoAbstract:Recently, Pyrazole Derivatives as high affinity and selective A2A adenosine receptor antagonists have been reported. But, so far, there are no reports about the inhibitory effects of multi-substituted Pyrazole Derivatives on apoptosis of vascular endothelial cells (VECs). In this study, we synthesized six Pyrazole Derivatives and characterized the structures of the compounds by IR, (1)H NMR, mass spectroscopy, and element analysis. The biology assay showed that a novel Pyrazole Derivative, ethyl 3-(o-chlorophenyl)-5-methyl-1-phenyl-1H-Pyrazole-4-carboxylate (MPD) at low concentration (25muM) increased VECs viability and inhibited VECs apoptosis induced by deprivation of serum and FGF-2. During this process, the levels of integrin beta4, reactive oxygen species (ROS), and p53 were depressed obviously. The data suggested that MPD was a potential inhibitor of apoptosis associated with the signal pathway mediated by integrin beta4, ROS, and p53 in VECs.
Avery August - One of the best experts on this subject based on the ideXlab platform.
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structural requirements for the inhibition of calcium mobilization and mast cell activation by the Pyrazole Derivative btp2
The International Journal of Biochemistry & Cell Biology, 2011Co-Authors: Mankit Law, Luis J Morales, Laurie F Mottram, Archana Iyer, Blake R Peterson, Avery AugustAbstract:Mast cells play a critical role in the development of the allergic response. Upon activation by allergens and IgE via the high affinity receptor for IgE (FcɛRI), these cells release histamine and other functional mediators that initiate and propagate immediate hypersensitivity reactions. Mast cells also secrete cytokines that can regulate immune activity. These processes are controlled, in whole or part, by increases in intracellular Ca(2+) induced by the FcɛRI. We show here that N-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-4-methyl-1,2,3-thiadiazole-5-carboxamide (BTP2), a Pyrazole Derivative, inhibits activation-induced Ca(2+) influx in the rat basophil cell line RBL-2H3 and in bone marrow-derived mast cells (BMMCs), without affecting global tyrosine phosphorylation of cellular proteins or phosphorylation of the mitogen-activated protein kinases Erk1/2, JNK and p38. BTP2 also inhibits activation-induced degranulation and secretion of interleukin (IL)-2, IL-3, IL-4, IL-6, IL-13, tumor necrosis factor (TNF)-α, and granulocyte macrophage-colony stimulating factor (GM-CSF) by BMMCs, which correlates with the inhibition of Nuclear Factor of Activated T cells (NFAT) translocation. In vivo, BTP2 inhibits antigen-induced histamine release. Structure-activity relationship analysis indicates that substitution at the C3 or C5 position of the Pyrazole moiety on BTP2 (5-trifluoromethyl-3-methyl-Pyrazole or 3-trifluoromethyl-5-methyl-Pyrazole, respectively) affected its activity, with the trifluoromethyl group at the C3 position being critical to its activity. We conclude that BTP2 and related compounds may be potent modulators of mast cell responses and potentially useful for the treatment of symptoms of allergic inflammation.
