Heterocyclic synthesis with nitriles: synthesis of pyridazine and pyridopyridazine derivatives [PDF]
The reaction of MND with aryldiazonium chlorides followed by cyclization afforded the pyridazinimine derivatives. Reaction of the latter with another mole of malononitrile produce only pyrido[3,2-c]pyridazine derivatives.
Campos, Ana M. F. Oliveira +2 more
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Functionalization of diazines and benzo derivatives through deprotonated intermediates. [PDF]
International audienceThis critical review targets as a readership researchers generally oriented toward organic synthesis and in particular those active in heterocyclic chemistry.
Chevallier, Floris, Mongin, Florence
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In the designed compounds, either a biarylamide or biarylurea moiety or an N-substituted piperazine motif was linked to position 1 of the phthalazine core. The anti-proliferative activity of the synthesised compounds revealed that eight compounds (6b, 6e,
Salwa Elmeligie +6 more
doaj +1 more source
Binding hotspots of BAZ2B bromodomain: Histone interaction revealed by solution NMR driven docking. [PDF]
Bromodomains are epigenetic reader domains, which have come under increasing scrutiny both from academic and pharmaceutical research groups. Effective targeting of the BAZ2B bromodomain by small molecule inhibitors has been recently reported, but no ...
Alessio Ciulli +37 more
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Synthesis and Spectral Characterization of Benzo[6,7] [1,5]diazocino[2,1-a]isoindol-12-(14H)-one Derivatives [PDF]
© 2016 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).A simple ...
Bassin +9 more
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Light‐Driven Catalyst‐Free Access to Phthalazines: Entry to Antiviral Model Drugs by Merging Domino Reactions** [PDF]
We report the development of a metal‐free four‐step one‐pot synthetic strategy to access high‐value functionalized phthalazines using o‐methyl benzophenones as starting compounds.
Guryev, Anton +8 more
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Designer Xanthone An Inhibitor Scaffold for MDR-Involved Human Glutathione Transferase Isoenzyme A1-1 [PDF]
Glutathione transferases (GSTs) are cell detoxifiers involved in multiple drug resistance (MDR), hampering the effectiveness of certain anticancer drugs.
Clonis, Yannis D. +7 more
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Bromodomains in Protozoan Parasites: Evolution, Function, and Opportunities for Drug Development [PDF]
Parasitic infections remain one of the most pressing global health concerns of our day, affecting billions of people and producing unsustainable economic burdens.
Huang, Sherri +3 more
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Selective modulators of α5-containing GABAA receptors and their therapeutic significance [PDF]
GABA receptors containing the α subunit (αGABARs) are found mainly in the hippocampus where they mediate a tonic chloride leak current and contribute a slow component to GABAergic inhibitory synaptic currents.
Lynch, Joseph W., Soh, Ming Shiuan
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Micro-RNAS that control myosin expression and myofiber identity [PDF]
The present invention relates to the identification of two microRNAs, miR-499 and miR-208b, that repress fast skeletal muscle contractile protein genes. Expression of miR-499 and/or miR-208b can be used to repress fast fiber genes and activate slow fiber
Olson, Eric N., van Rooij, Eva
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