- Oxalic amide ligands, and uses thereof in copper-catalyzed coupling reaction of aryl halides
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The present invention provides oxalic amide ligands and uses thereof in copper-catalyzed coupling reaction of aryl halides. Specifically, the present invention provides a use of a compound represented by formula I, wherein definitions of each group are described in the specification. The compound represented by formula I can be used as a ligand in copper-catalyzed coupling reaction of aryl halides for the formation of C—N, C—O and C—S bonds.
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Page/Page column 85-86
(2020/01/09)
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- 4-AZAPODOPHYLOTOXINS COMPOUNDS
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The present disclosure relates to 4-azapodophylotoxins compounds, pharmaceutical compositions comprising such compounds, kits, and methods for using such compounds or pharmaceutical compositions.
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Page/Page column 62-63
(2017/09/15)
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- Antineoplastic Agents. 585. Isolation of Bridelia ferruginea Anticancer Podophyllotoxins and Synthesis of 4-Aza-podophyllotoxin Structural Modifications
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Cytotoxic constituents of the terrestrial plant Bridelia ferruginea were isolated using bioactivity-guided fractionation, which revealed the presence of the previously known deoxypodophyllotoxin (1), isopicrodeoxypodophyllotoxin (2), β-peltatin (3), β-pel
- Pettit, George R.,Searcy, Justin D.,Tan, Rui,Cragg, Gordon M.,Melody, Noeleen,Knight, John C.,Chapuis, Jean-Charles
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p. 507 - 518
(2016/04/19)
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- CuI/Oxalic Diamide Catalyzed Coupling Reaction of (Hetero)Aryl Chlorides and Amines
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A class of oxalic diamides are found to be effective ligands for promoting CuI-catalyzed aryl amination with less reactive (hetero)aryl chlorides. The reaction proceeds at 120 °C with K3PO4 as the base in DMSO to afford a wide range of (hetero)aryl amines in good to excellent yields. The bis(N-aryl) substituted oxalamides are superior ligands to N-aryl-N′-alkyl substituted or bis(N-alkyl) substituted oxalamides. Both the electronic nature and the steric property of the aromatic rings in ligands are important for their efficiency.
- Zhou, Wei,Fan, Mengyang,Yin, Junli,Jiang, Yongwen,Ma, Dawei
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supporting information
p. 11942 - 11945
(2015/10/06)
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- Identification of the first inhibitor of the GBP1:PIM1 interaction. Implications for the development of a new class of anticancer agents against paclitaxel resistant cancer cells
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Class III β-tubulin plays a prominent role in the development of drug resistance to paclitaxel by allowing the incorporation of the GBP1 GTPase into microtubules. Once in the cytoskeleton, GBP1 binds to prosurvival kinases such as PIM1 and initiates a sig
- Andreoli, Mirko,Persico, Marco,Kumar, Ajay,Orteca, Nausicaa,Kumar, Vineet,Pepe, Antonella,Mahalingam, Sakkarapalayam,Alegria, Antonio E.,Petrella, Lella,Sevciunaite, Laima,Camperchioli, Alessia,Mariani, Marisa,Di Dato, Antonio,Novellino, Ettore,Scambia, Giovanni,Malhotra, Sanjay V.,Ferlini, Cristiano,Fattorusso, Caterina
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p. 7916 - 7932
(2014/12/10)
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- Synthesis of novel functionalized 4-aza-2,3-didehydropodophyllotoxin derivatives with potential antitumor activity
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Novel arylamino alcohols were synthesized and these alcohols were used to prepare 12 novel N-(2-hydroxy-ethyl)-2,3-didehydroazapodophyllotoxins, in one step, by simple reflux in ethanol. Isolated yields in the range of 50-70% were obtained.
- Kumar, Ajay,Alegria, Antonio E.
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experimental part
p. 1275 - 1282
(2011/02/21)
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- Dihydrofuro[3,4-b]quinolin-1-one compounds
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The invention relates to compound of formula (I): wherein: represents a single or double bond, R0represents hydrogen or hydroxy or alkoxy, R1and R2, which are identical or different, each represents hydrogen or halogen or alkyl, alkoxy, hydroxy, polyhaloalkyl, nitro or optionally substituted amino or ?wherein m represents an integer such that 1≦m≦4, or form together with the carbon atoms carrying them an aromatic or non-aromatic, mono- or bi-cyclic group having from 5 to 12 ring members and optionally containing 1 or 2 hetero atoms selected from O, S and N, R3represents hydrogen or aryl, heteroaryl, cycloalkyl, optionally substituted alkyl or a group of formula COR7wherein R7represents aryl, optionally substituted alkyl, optionally substituted amino or OR10wherein R10represents aryl or optionally substituted alkyl, X represents oxygen or sulphur or —CH2— or —CH2—CH2—, Ar represents aryl, heteroaryl or arylalkyl, its optical isomers, its hydrates, solvates, and also its addition salts with a pharmaceutically acceptable acid. Medicinal products containing the same are useful in the treatment of cancer.
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