- Asymmetric [3 + 3] Annulation of Copper-Allenylidenes with Pyrazolones: Synthesis of Chiral 1,4-Dihydropyrano[2,3- c]pyrazoles
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The copper-catalyzed asymmetric [3 + 3] annulation of ethynyl benzoxazinanones with pyrazolones has been achieved, providing simple access to 1,4-dihydropyrano[2,3-c]pyrazole derivatives in moderate to excellent yields with excellent enantioselectivities (up to 99% ee). Compared with previous annulation reactions of copper-allenylidenes from ethynyl benzoxazinanones, the current reaction fused the three carbon atoms of the propargyl moiety into a heterocyclic framework.
- Jiang, Feng,Feng, Xinping,Wang, Rou,Gao, Xing,Jia, Hao,Xiao, Yumei,Zhang, Cheng,Guo, Hongchao
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supporting information
p. 5278 - 5281
(2018/09/13)
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- Anti-cancer compounds targeting Ral GTPases and methods of using the same
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The invention provides methods of inhibiting the growth or metastasis of a cancer in a mammal by inhibiting a Ral GTPase in the mammal. The invention also provides small molecule inhibitors of Ral GTPases useful in the methods of the invention and pharmaceutical compositions containing the therapeutically effective compounds of the invention, and methods of using the same.
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Page/Page column 55; 64
(2016/06/28)
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- ANTI-CANCER COMPOUNDS TARGET RAL GTPASES AND METHODS OF USING THE SAME
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Methods of inhibiting the growth or metastasis of a cancer in a subject by inhibiting a Ral GTPase in the subject, and small molecule inhibitors of Ral GTPases useful in the methods of the invention. Pharmaceutical compositions containing the compounds of the invention, and methods of using the same.
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Page/Page column 37
(2016/04/26)
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- Synthesis of novel Ral inhibitors: An in vitro and in vivo study
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Chemical synthesis was performed to produce a series of 6-amino-1,3-disubstituted-4-phenyl-1,4-dihydro pyrano[2,3-c]pyrazole-5-carbonitrile compounds (14–57) which were characterized by1H NMR,13C NMR and LC/MS–MS. These compounds were assessed for their effect on the in vitro anchorage independent growth of human lung cancer cell line H2122 and IC50values calculated. Two of the more potent compounds, BQU057 40 and BQU082 57 also displayed a dose dependent effect on RalA and RalB activity in H2122 spheroids using the common RalBP1 pull-down assay. Mouse PK and tissue distribution studies on 40 and 57 were performed and demonstrated that parent drug was present in tumor 3.0 h post ip (50 mg/Kg) dose.
- Yan, Chao,Theodorescu, Dan,Miller, Bettina,Kumar, Amit,Kumar, Vijay,Ross, David,Wempe, Michael F.
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supporting information
p. 5815 - 5818
(2016/11/25)
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- P-Toluenesulphonic acid-promoted, I2-catalysed sulphenylation of pyrazolones with aryl sulphonyl hydrazides
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Aryl pyrazolone thioethers were synthesized via the I2-catalysed cross-coupling of pyrazolones with aryl sulphonyl hydrazides in the presence of p-toluenesulphonic acid, which has been proposed to promote the reaction by facilitating the decomposition of sulphonyl hydrazides. This journal is
- Zhao, Xia,Zhang, Lipeng,Li, Tianjiao,Liu, Guiyan,Wang, Haomeng,Lu, Kui
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supporting information
p. 13121 - 13123
(2014/12/11)
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- ANTI-CANCER COMPOUNDS TARGETING RAL GTPASES AND METHODS OF USING THE SAME
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The invention provides methods of inhibiting the growth or metastasis of a cancer in a mammal by inhibiting a Ral GTPase in the mammal. The invention also provides small molecule inhibitors of Ral GTPases useful in the methods of the invention and pharmaceutical compositions containing the therapeutically effective compounds of the invention, and methods of using the same.
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Page/Page column 40; 41; 52; 53
(2013/07/05)
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- Synthesis of new pyrazolone dyes
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New azo- and bisazo-5-pyrazolone dyes have been synthesised by azo coupling of various arylamines and aryl diamines with 5-pyrazolones: 1-methyl-3-phenyl-1H-pyrazol-5(4H)-one, 1-(4-chlorophenyl)-3-isopropyl-1H- pyrazol- 5(4H)-one and 3-isopropyl-1-(4-methoxyphenyl)-1H-pyrazol-5(4H)-one, respectively. All new synthesised dyes have been characterised by FTIR, 1H, 13C NMR and UV-Vis spectral studies with GC/MS and LC/MS analyses. FTIR and 1H NMR studies confirmed the existence of azo- and hydrazo-tautomeric forms of the dyes in the solid and liquid states, respectively.
- Gunkara, Omer Tahir,Bagdatli, Emine,Ocal, Nuket
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p. 227 - 231
(2013/07/27)
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- DRUGS COMPRISING COMBINATION OF ANTITHROMBOTIC AGENT WITH PYRAZOLONE DERIVATIVE
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It is intended to provide drugs for treating and/or preventing ischemic diseases which are safe and have little side effects. Namely, drugs comprising a combination of an antithrombotic agent and a pyrazolone derivative defined in the description or its pharmaceutically acceptable salt.
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- 2-(pyrazol-5-yl-oxymethyl)-1,2-benzisothiazol-3 (2H)-One 1, 1-dioxides and compositions and method of use thereof
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2-(Pyrazol-5-yl-oxymethyl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxides, pharmaceutical compositions containing them and methods for the treatment of degenerative diseases utilizing them.
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- Novel 1,2-dialkylpyrazolium compounds having 3-(or 3,5-) nitrogen-containing heterocyclic group as herbicides
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There are provided 1,2-dialkylpyrazolium compounds having positioned thereon a 3- or 5-substituted nitrogen-containing heterocyclic group or 3,5-disubstituted nitrogen-containing heterocyclic groups as well as a method for preparing the same. There is als
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- 1,2-Dialkyl-3(or 3,5)-N-heterocyclic pyrazolium salts of derivatives thereof as fungicidal agents
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There is provided a method for controlling fungi with a fungicidally effective amount of a 1,2-dialkyl-3(or 3,5)-N-heterocyclic pyrazolium salt. There is also provided a method for protecting living plants from attack by fungi through the application to t
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