Search results for "combinatorial"
showing 10 items of 1208 documents
Haptens, bioconjugates, and antibodies for penthiopyrad immunosensing
2014
4 pages, 1 table, 2 figures.
Forchlorfenuron-mimicking haptens: From immunogen design to antibody characterization by hierarchical clustering analysis
2011
To obtain highly-specific and selective forchlorfenuron binders, a collection of functionalized derivatives with different spacer arm locations and lengths was prepared. By immunization with target-mimicking haptens, a large battery of monoclonal and polyclonal antibodies against this synthetic cell regulator was produced and exhaustively characterized in two immunoassay formats using homologous and heterologous conjugates. Antibodies with IC50 values lower than 0.3 nM were successfully raised from the prepared immunogens, thus evidencing the efficacy of the explored strategies. In order to identify significant epitopes in the antibody-antigen interaction, a series of new chemical forchlorf…
Chemistry of detrifluoroacetylativelyin situgenerated fluoro-enolates
2018
This review article comprehensively profiles all literature reports (2015-2018) related to the detrifluoroacetylative in situ generation of fluorine-containing enolates and their reactions with electrophilic reagents. The innovative facets of this unconventional methodology and its synthetic generality for the preparation of fluorine-containing compounds of high medicinal value are highlighted.
A Novel Enzyme-Triggered Domino Reaction Producing Fluorescent Quinoxalin-2(1H)-One-Based Heterocycles
2020
A simple and effective biocompatible domino reaction triggered by a model protease and leading to formation of strongly fluorescent quinoxalin-2(1H)-one N-heterocycles is described. Some positive attributes including versatility and ability to provide outstanding fluorescence "OFF-ON" responses were revealed by this work. They open the way for practical applications of this novel type of "covalent-assembly" based fluorescent probes in the fields of sensing and bioimaging.; A simple and effective biocompatible domino reaction triggered by a model protease and leading to formation of strongly fluorescent quinoxalin-2(1H)-one N-heterocycles is described. Some positive attributes including vers…
BODIPYS and aza-BODIPY derivatives as promising fluorophores for in vivo molecular imaging and theranostic applications
2019
Since their discovery in 1968, the BODIPYs dyes (4,4-difluoro-4-bora-3a, 4a diaza-s-indacene) have found an exponentially increasing number of applications in a large variety of scientific fields. In particular, studies reporting bioapplications of BODIPYs have increased dramatically. However, most of the time, only in vitro investigations have been reported. The in vivo potential of BODIPYs and aza-BODIPYs is more recent, but considering the number of in vivo studies with BODIPY and aza-BODIPY which have been reported in the last five years, we can now affirm that this family of fluorophores can be considered important as cyanine dyes for future in vivo and even clinical applications. Thi…
Design and synthesis of 1-aryl-5-anilinoindazoles as c-Jun N-terminal kinase inhibitors.
2012
Starting from pyrazole HTS hit (1), a series of 1-aryl-1H-indazoles have been synthesized as JNK3 inhibitors with moderate selectivity against JNK1. SAR studies led to the synthesis of 5r as double digital nanomolar JNK3 inhibitor with good in vivo exposure.
Hydroxy-Directed Enantioselective Hydroxyalkylation in the Carbocyclic Ring of Indoles
2017
[EN] A Cinchona-derived squaramide catalyzes the reaction between hydroxyindoles and isatins leading to enantioenriched indoles substituted in the carbocyclic ring. The reaction proceeds efficiently with differently substituted isatins, yielding the desired products with excellent regioselectivity, good yields, and high enantiocontroi. Moreover, every position of the carbocyclic ring of the indole can be functionalized by using the appropriate starting hydroxyindole. The OH group was removed smoothly upon hydrogenolysis of the corresponding triflate.
Straight Access to Indoles from Anilines and Ethylene Glycol by Heterogeneous Acceptorless Dehydrogenative Condensation.
2017
The development of original strategies for the preparation of indole derivatives is a major goal in drug design. Herein, we report the first straight access to indoles from anilines and ethylene glycol by heterogeneous catalysis, based on an acceptorless dehydrogenative condensation, under noninert conditions. In order to achieve high selectivity, a combination of Pt/Al2O3 and ZnO have been found to slowly dehydrogenate ethylene glycol generating, after condensation with the amine and tautomeric equilibrium, the corresponding pyrrole-ring unsubstituted indoles.
Selektive Synthesen zu 1?-aryl-, 1?-hetaryl-und 1?-alkylsubstituierten 3-Vinylindolen
1987
Selective methods for deriving 1′-aryl-, 1′-indolyl-, 1′-pyrrolyl- and 1′-methyl-substituted 3-vinylindoles2 are described. In all cases the precursors were 3-acylindoles. The new compounds are synthetically useful synthons for annelation of the indole skeleton.
Nucleophilic reactions in the indole series: displacement of bromine under phase transfer catalysis
2008
A novel synthetic approach for the synthesis of 3-substituted indoles by nucleophilic substitution of 3-bromo derivatives under phase transfer catalysis (PTC) was reported.