Fluorescein isothiocyanate incorporated in the immunofluorescent antibody test system used for serodiagnpsis of leishmanial and other infections suffers certain inherent disadvantages. Aminomethyl coumarin acetic acid, a new fluorescent label for protein, yields better results regarding non-spec...
The synthesis of 1-phenylpyrazolin-5-one carboxylate esters of biotin and fluorescein and their specific reactivity with amines under mild conditions to label various synthetic biopolymers such as oligonucleotides, peptides and PNA's is described.
This Letter describes the synthesis and properties of double-stranded antisense oligonucleotides connected with a pentaerythritol linker. We found that double-stranded antisense oligonucleotides with aminomethyl residues have high affinity for single-stranded DNA or RNA in buffer solutions with ...
A new class of fluorescein derivatives with chemically reactive amino and N-alkylamino “arms” in the 4′-position were synthesized and their utility in the development of fluorescence polarization immunoassays (FPIA) for cortisol and estriol was evaluated. The positioning of the arm in one of ...
The fluorescein derivants (Fluorescein: (2-(6-Hydroxy-3-oxo-(3H)-xanthen-9-yl) benzoic acid), Fluorescein-DA: (Bis [N,N-bis (carboxymethyl) aminomethyl] fluorescein) and Fluorescein-DAFe(III): (Bis [N,N-bis (carboxymethyl) aminomethyl] fluoresceinFerrous(III)) with a tricyclic plane structure we...
The interaction of DNA with Bis [N,N-bis (carboxymethyl) aminomethyl] fluorescein-Ferrous(III) (Fluorescein-DA-Fe(III)) with dual functional (sonodynamic and sonocatalytic) activity was studied by UV–vis spectroscopy, fluorescence spectroscopy, FT-IR spectroscopy, circular dichroism (CD) spectr...
The carbonyl cobalt complex Cp*Co(CO)I2 catalyzes carbenoid Co alkylation of N-(pyrimidin-2-yl)indole with methyl 3,3,3-trifluoro-2-diazopropionate regioselectively giving 2-substituted indole, while the N,N’-ligated cations [CpCo(L)I]+ (L = bipy, phen) provide 3-substitution exclusively. The s...
Pyrimidin-2-yl tosylates which are successfully applied as the electrophiles instead of halides coupled with olefins via Pd(PPh3)2Cl2 catalyzed Mizoroki–Heck reaction conditions to give the corresponding C2-alkenyl pyrimidine derivatives with high β-regioselectivity. This protocol proves to be...
A metal-free synthesis of pyrimidine functionalized primary amines via direct amination of pyrimidin-2-yl tosylate with aqueous ammonia has been developed under mild conditions. The desired products pyrimidin-2-amines can be generated in excellent yields in PEG-400, without any catalysts or othe...
The Janus kinase (JAK) family of tyrosine kinases has been proven to provide targeted immune modulation. Orally available JAK inhibitors have been used for the treatment of immune-mediated inflammatory diseases, such as rheumatoid arthritis (RA). Here, we report the design, synthesis and biologi...
Gain-of-function mutation in isocitrate dehydrogenase 1 (IDH1) is closely related to certain human cancers and is emerging as an attractive antitumor target. However, developing safe and effective inhibitors of mutant IDH1 (mIDH1) are facing many challenges. In this study, an integrated computat...
We have demonstrated a simple, green, and environmentally friendly approach for the synthesis of polystyrene-supported gold ([email protected]) nanoparticles by using Schisandra chinensis fruit extract through a novel chemical route. The prepared [email protected] NPs have been well characterize...
Translocator protein (TSPO) expression is closely related with neuroinflammation and neuronal damage which might cause several central nervous system diseases. Herein, a series of TSPO ligands (11a–c and 13a–d) with a 2-phenylpyrazolo[1,5-a]pyrimidin-3-yl acetamide structure were prepared and ...
4-(4-Hexyloxyphenyl)-2,6-di(pyrazin-2-yl)pyridine (1), an analogue of the archetypal ligand, 2,2′:6′,2″-terpyridine containing additional outer N-donating sets is synthesized through the facile one-step Kröhnke condensation reaction. It is observed that different crystallization conditions af...
Oesophageal adenocarcinoma (OAC) is an aggressive disease with 5-year survival rates of
Three new supramolecular complexes based on a 2-(pyrazin-2-yl)-1H-benzimidazole (Hpbi) and a series of Cd(II) salts have been solvothermally synthesized and structurally characterized by single-crystal X-ray diffraction analysis. Reaction of CdCl2·2.5H2O with Hpbi afforded a one-dimensional cha...
The organic compound 1-(pyrazin-2-yl) piperidin-2-ol (abbreviated as PPOL) has been synthesized and characterized by IR, Raman, 1H NMR and UV–Vis spectroscopy. The Fourier-transform Raman (3500–50 cm−1) and infrared spectra (4000–400 cm−1) were recorded in the solid state and interpreted by c...
The three Pim kinases are a small family of serine/threonine kinases regulating several signaling pathways that are fundamental to tumorigenesis. As such, the Pim kinases are a very attractive target for pharmacological inhibition in cancer therapy. Herein, we describe our efforts toward the dev...
A simple and highly efficient metal-free method for the synthesis of 2-(pyrazin-2-yl)benzimidazoles has been developed on the basis of the novel ring contraction of 3-aroyl- and 3-alkanoylquinoxalin-2-ones with diaminomaleonitrile.
PB2 is an important subunit of influenza RNA-dependent RNA polymerase (RdRP) and has been recognized as a promising target for the treatment of influenza. We herein report the discovery of a new series of PB2 inhibitors containing the skeleton 5-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)pyrazin-2(...
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