104765-26-6Relevant articles and documents
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
Zhao, Bao-Xiang,Zhang, Lu,Zhu, Xing-Shang,Wan, Mao-Sheng,Zhao, Jing,Zhang, Yun,Zhang, Shang-Li,Miao, Jun-Ying
, p. 5171 - 5180 (2008/12/20)
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.
Synthesis of Substituted N-Hydroxylactams, Lactams, Quinoline-N-oxides, and Quinolines by Catalyzed Reductive Cyclization of 2-Nitrocinnamoyl Derivatives with Hydrogen/Platinum Black
Sicker, D.,Rabe, A.,Zakrzewski, A.,Mann, G.
, p. 1063 - 1070 (2007/10/02)
Substituted nitrobenzenes 1a-1m, consisting of two series of 6 analogous compounds, containing the structural unit of an α,β-substituted 2-nitrocinnamoyl group have been reductively cyclized by means of hydrogen in the presence of platinum black catalyst to form four types of heterocycles: N-hydroxylactams 2a and b, lactams 3 and 4, quinoline-N-oxides 5a-d, and quinolines 6a and b.The type of substituents at the 2-nitrocinnamoyl group is of significance for the type of heterocycle formed in this reaction.It is of special interest that by the use of the reduction system hydrogen/platinum black the probability to obtain N-hydroxylactams or quinoline-N-oxides, which are difficult to obtain by alternative procedures, becomes much higher than by the use of many reducing agents noncatalytically.
