- BRD4-JAK2 INHIBITORS
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Disclosed herein are compounds that are inhibitors of BDR4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BDR4 are also disclosed. In certain aspects, disclosed are compounds of Formula I through IV.
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Page/Page column 141
(2020/03/29)
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- Fluorescence Properties and Exciplex Formation of Emissive Naphthyridine Derivatives: Application as Sensors for Amines
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Water-soluble donor–acceptor-type fluorophore 15Nap-Cl having two trifluoromethyl groups and a Cl group on a 1,5-aminonaphthyridine framework was prepared. Fluorophore 15Nap-Cl showed strong solvatochromic fluorescence, and, as the solvent polarity increased, a bathochromic shift was observed accompanied by an increase in the fluorescence quantum yield. In addition, in the presence of amines such as ethylamine, diethylamine, and aniline, further considerable bathochromic shifts in the fluorescence were observed. Density functional calculations identified the source of the fluorescence behavior as exciplex formation between 15-Nap-Cl and the corresponding amine. The fluorescence behavior was exploited to fabricate a sensor that can identify various primary, secondary, and tertiary amines.
- Hirota, Junko,Usui, Kazuteru,Fuchi, Yasufumi,Sakuma, Masaomi,Matsumoto, Shota,Hagihara, Ryusuke,Karasawa, Satoru
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p. 14943 - 14952
(2019/11/13)
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- A modular approach to synthetic RNA binders of the hepatitis C virus internal ribosome entry site
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(Figure Presented) DAPper ligands: The 3,5-diaminopiperidine (DAP) heterocycle has been developed as a structural mimetic of the RNA-recognizing pharmacophore of the 2-DOS scaffold. Here we describe the synthesis of novel modular DAP ligands that bind to a conformational target in the internal ribosome entry site RNA of the hepatitis C virus.
- Carnevali, Maia,Parsons, Jerod,Wyles, David L.,Hermann, Thomas
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scheme or table
p. 1364-1367+1315
(2011/04/24)
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- Pyridonecarboxylic acid derivatives or their salts and antibacterial agent comprising the same as the active ingredient
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A pyridonecarboxylic acid derivative represented by the following general formula (1): STR1 [wherein R1 represents hydrogen atom or a carboxyl protective group; R2 represents hydroxyl group, a lower alkoxy group, or a substituted or unsubstituted amino group; R3 represents hydrogen atom or a halogen atom; R4 represents hydrogen atom or a halogen atom; R5 represents a halogen atom or an optionally substituted saturated cyclic amino group; R6 represents hydrogen atom, a halogen atom, nitro group, or an optionally protected amino group; X, Y and Z may be the same or different and respectively represent nitrogen atom, --CH= or --CR7 = (wherein R7 represents a lower alkyl group, a halogen atom, or cyano group) (with the proviso that at least one of X, Y and Z represent the nitrogen atom), and W represents nitrogen atom or --CR8 = (wherein R8 represents hydrogen atom, a halogen atom, or a lower alkyl group)] or its salt, as well as an antibacterial agent containing such compound are provided.
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