- Synthesis of Pyridoclax Analogues: Insight into Their Druggability by Investigating Their Physicochemical Properties and Interactions with Membranes
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Pyridoclax is considered a promising anticancer drug, acting as a protein-protein interaction disruptor, with potential applications in the treatment of ovarian, lung, and mesothelioma cancers. Eighteen sensibly selected structural analogues of Pyridoclax
- De Pascale, Martina,Iacopetta, Domenico,Since, Marc,Corvaisier, Sophie,Vie, Véronique,Paboeuf, Gilles,Hennequin, Didier,Perato, Serge,De Giorgi, Marcella,Sinicropi, Maria Stefania,Sopkova-De Oliveira Santos, Jana,Voisin-Chiret, Anne-Sophie,Malzert-Freon, Aurélie
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p. 136 - 154
(2019/12/15)
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- Imidazole derivatives, its pharmaceutical composition and use thereof
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Imidazolone compounds, pharmaceutically acceptable salts, solvates, polymorphs or prodrugs thereof are disclosed. Pharmaceutical compositions comprising above substances and uses for preventing and treating protein kinases related diseases, such as cancers, metabolic diseases, cardiovascular diseases and the like, are also disclosed.
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Paragraph 0227-0229
(2017/02/24)
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- Compound containing quinoxaline and pyridine groups and organic electroluminescent device thereof
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The invention provides an organic electroluminescent compound containing quinoxaline and pyridine groups. The compound has better heat stability, high luminous efficiency and high luminous purity, can be used for manufacturing an organic electroluminescent device, and is applied to the field of organic solar cells, organic thin film transistors or organic photoreceptors. The invention also provides the organic electroluminescent device, which comprises an anode, a cathode and an organic layer, wherein the organic layer includes more than one layer in a luminous layer, a hole injection layer, a hole transporting layer, a hole blocking layer, and electron injection layer and an electron transporting layer; at least one layer in the organic layer contains a compound as shown by a structural formula I which is as shown in the description.
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Paragraph 0065; 0066
(2016/10/08)
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- Molecular design of high-molecular-orientation electron-transport materials and application to organic light-emitting diodes
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Two novel electron-transport materials (ETMs), 2,3′-Bpy- TP and 2,4′-Bpy-TP, with high horizontal molecular orientation to substrates, were synthesized. It was shown by measuring the IR absorption spectra of their deposited thin films that C-H N hydrogen bonds are formed between the 2,3′-Bpy-TP molecules and between the 2,4′-Bpy-TP molecules. It was also shown that there is a closed relationship between their molecular orientations and the driving voltages of electron-only devices (EODs) using them as electron-transport layers (ETLs).
- Togashi, Kazunori,Sagara, Yuta,Yasuda, Takuma,Adachi, Chihaya
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supporting information
p. 651 - 653
(2013/07/27)
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- Structural characterizations of oligopyridyl foldamers, α-helix mimetics
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Protein-protein interactions are central to many biological processes, from intracellular communication to cytoskeleton assembly, and therefore represent an important class of targets for new therapeutics. The most common secondary structure in natural proteins is an α-helix. Small molecules seem to be attractive candidates for stabilizing or disrupting protein-protein interactions based on α-helices. In our study, we assessed the ability of oligopyridyl scaffolds to mimic the α-helical twist. The theoretical as well as experimental studies (X-ray diffraction and NMR) on conformations of bipyridines in the function of substituent and pyridine nitrogen positions were carried out. Furthermore, the experimental techniques showed that the conformations observed in bipyridines are maintained within a longer oligopyridyl scaffold (quaterpyridines). The alignment of the synthesized quaterpyridine with two methyl substituents showed that it is an α-helix foldamer; their methyl groups overlap very well with side chain positions, i and i + 3, of an ideal α-helix.
- Sopkova-De Oliveira Santos, Jana,Voisin-Chiret, Anne Sophie,Burzicki, Gregory,Sebaoun, Laure,Sebban, Muriel,Lohier, Jean-Francois,Legay, Remi,Oulyadi, Hassan,Bureau, Ronan,Rault, Sylvain
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scheme or table
p. 429 - 439
(2012/06/18)
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- LINCOSAMIDE DERIVATIVE, AND ANTIBACTERIAL AGENT COMPRISING THE SAME AS ACTIVE INGREDIENT
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An objective of the present invention is to provide compounds of formula (I) or their pharmacologically acceptable salts or solvates wherein A represents aryl while R1 represents a five- or six-membered monocyclic heterocyclic group, or A represents a four- to six-membered monocyclic heterocyclic group while R1 represents aryl or a five- or six-membered monocyclic heterocyclic group; R2 represents a hydrogen atom or C1-6 alkyl; R3 represents C1-6 alkyl or C3-6 cycloalkyl-C1-4 alkyl; R4, R5, and R6 represent a hydrogen atom; R7 represents C1-6 alkyl; and m is 1 to 3. The compounds are novel lincosamide derivatives that have a potent activity against resistant Streptococcus pneumoniae. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.
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Page/Page column 24
(2010/04/24)
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- 2-Pyridyl and 3-pyridylzinc bromides: direct preparation and coupling reaction
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A facile synthetic approach to the direct preparation of 2-pyridyl and 3-pyridylzinc bromides has been demonstrated using Rieke zinc with 2-bromopyridine and 3-bromopyridine, respectively. A variety of different electrophiles have been coupled with the resulting organozinc reagents to give the corresponding cross-coupling products in moderate to good yields.
- Kim, Seung-Hoi,Rieke, Reuben D.
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experimental part
p. 3135 - 3146
(2010/06/13)
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- A facile synthetic approach to the preparation of 3-pyridyl derivatives: Preparations and coupling reactions of 3-pyridylzinc and its analogues
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A facile synthetic approach to the direct preparation of 3pyridylzinc bromide has been demonstrated using Rieke zinc with 3-bromopyridine in the presence of a catalytic amount of lithium chloride. A variety of different electrophiles have been coupled to give the corresponding cross-coupling products in moderate to good yields. Also, this methodology has been expanded to the preparation of the corresponding organozinc reagents of 3-bromopyridine analogues. Georg Thieme Verlag Stuttgart.
- Kim, Seung-Hoi,Slocum, Tim B.,Rieke, Reuben D.
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experimental part
p. 3823 - 3827
(2010/03/04)
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- Synthesis of dihalo bi- and terpyridines by regioselective Suzuki-Miyaura cross-coupling reactions
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This paper describes an efficient and regioselective synthetic route leading to new dihalobi- and terpyridines. We developed a strategy based on regioselective sequence of Suzuki-Miyaura cross-coupling reactions between bromopyridyl boronic acids and dihalopyridines and dihalobipyridines. The study of the influence of the nature and the position of the halogen atoms leads to prepare bromoiododerivatives to obtain good selectivities.
- Burzicki, Grégory,Voisin-Chiret, Anne Sophie,Oliveira Santos, Jana Sopkovà-de,Rault, Sylvain
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experimental part
p. 5413 - 5417
(2009/10/24)
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- HYDANTOIN DERIVATIVES FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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This invention relates to compounds of the Formula: (I); or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-α or combinations thereof.
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Page/Page column 160
(2008/06/13)
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- ELECTRON TRANSPORTING MATERIAL AND ORGANIC ELECTROLUMINESCENT DEVICE USING THE SAME
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A compound represented by the formula (1):wherein G represents a n-valent linker group; n represents an integer of 2 to 4; R1 to R4 independently represent a hydrogen, a univalent group or a free atomic valency binding to the group G; and R5 to R8 independently represent a hydrogen or a univalent group; provided that any one of R1 to R4 is a free atomic valency binding to the group G, and n's 2,3'-bipyridyl groups may be the same as or different from one another. The compound is useful as an electron transporting material for an organic electroluminescent device. An organic electroluminescent device having the compound in the electron transporting layer shows a long operating life and a low driving voltage.
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Page/Page column 66
(2008/06/13)
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- Imidazolyl and pyrazolyl ethyne compounds
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In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted, unsaturated five, six or seven membered heterocyclic ring that includes at least one nitrogen atom and a
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- Cross-coupling between 3-pyridylmagnesium chlorides and heteroaromatic halides
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Phenyl- and thienylpyridines were prepared by Pd(0)-catalyzed cross-coupling of 3-pyridylmagnesium chlorides with iodobenzene or iodothiophene at room temperature. Starting from bromo and chloro azines and diazines, the Ni(0)-catalyzed reaction proved more suitable to allow the synthesis of pyridylpyridines, pyridylquinolines and pyridyldiazines.
- Bonnet, Véronique,Mongin, Florence,Trécourt, Fran?ois,Breton, Gilles,Marsais, Francis,Knochel, Paul,Quéguiner, Guy
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p. 1008 - 1010
(2007/10/03)
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