Contilistat, a new polyfunctionalized histone deacetylase inhibitor, showing potential capacity to inhibit cholinesterase/monoamine oxidase enzymes, and modulate histamine 3, sigma 1, 5-HT6 and dopamine 3 receptors for the treatment of cancer and neurodegenerative diseases [PDF]
The present work describes the design, and synthesis of the polyfunctionalized indole derivative Contilistat for the treatment of a broad diversity of cancers, and neurodegenerative diseases such as glioblastoma, and Alzheimer’s disease (AD). Contilistat
Ander, Matheu +10 more
core +2 more sources
Synthesis and cyclization reactions of 2-(6-methylquinolin-4-yl)malononitriles and ethyl 2-cyano-2-(6-methylquinolin-4-yl)acetates [PDF]
The nucleophilic substitution reactions of 2,4-dichloro-6-methylquinoline (1) and 4-chloro-6-methylquinolin-2(1H)-one (7) with malononitrile and ethyl cyanoacetate are described. The quinolinylmalononitrile 8a and cyanoacetate 8b were utilized to prepare
MOSTAFA M. ISMAIL
doaj +3 more sources
Site-Specific Surface Modification via Chemoselective Click Reactions on Cyclobutene-Functionalized Monolayers. [PDF]
ABSTRACT We report the first example of self‐assembled monolayers (SAMs) incorporating a cyclobutene‐substituted alkanethiol on a gold surface and the efficient modification of these monolayers via inverse electron‐demand Diels–Alder (IEDDA) cycloadditions.
Evans BW +5 more
europepmc +2 more sources
Evaluating Cellular Polyfunctionality with a Novel Polyfunctionality Index
Functional evaluation of naturally occurring or vaccination-induced T cell responses in mice, men and monkeys has in recent years advanced from single-parameter (e.g. IFN-γ-secretion) to much more complex multidimensional measurements. Co-secretion of multiple functional molecules (such as cytokines and chemokines) at the single-cell level is now ...
Larsen, Martin +5 more
openaire +5 more sources
Sequential reactions of aminoalkynes represent a powerful tool to easily assembly biologically important polyfunctionalized nitrogen heterocyclic scaffolds.
Antonio Arcadi +2 more
doaj +1 more source
Anomeric Amides: Valuable Reagents in Synthetic Organic Chemistry. [PDF]
Enabling late‐stage transformations and skeletal editing, anomeric amides have recently emerged as powerful synthetic tools. Due to their unique properties, anomeric amides have been employed in reactions ranging from amination to halogenation. This minireview provides an overview of recent progress in using anomeric amides across a variety of ...
Garg A, Vigier J, Lebel H, Besset T.
europepmc +3 more sources
Nowadays, most stroke patients are treated exclusively with recombinant tissue plasminogen activator, a drug with serious side effects and limited therapeutic window. For this reason, and because of the known effects of oxidative stress on stroke, a more
Daniel Diez-Iriepa +8 more
doaj +1 more source
Contilisant+Belinostat hybrids, as new multi-target-directed polyfunctionalized indole derivatives able to inhibit histone deacetylase/cholinesterase/monoamine oxidase enzymes, and modulate histamine 3/sigma 1/5-HT6/dopamine 3 receptors for the treatment of cancer and neurodegenerative diseases [PDF]
Herein we describe the design and synthesis of Contilisant+Belinostat hybrids as polyfunctionalized indole derivatives for the treatment of a broad diversity of cancers and neurodegenerative diseases, such as glioblastoma, and Alzheimer’s disease (AD ...
Ander, Matheu +9 more
core +2 more sources
Borylcyclopropanes: Synthetic Strategies and Applications
Borylcyclopropanes (cyclopropanes bearing a boron substituent) sit at the intersection of two privileged frameworks in synthesis. This review provides the first exhaustive survey of their chemistry, spanning metal–carbene, nucleophilic cyclization, radical, hydroboration, and C─H activation routes, and documenting applications in medicinal chemistry ...
Aiza A. Butt, Joseph M. Ready
wiley +2 more sources
Affix polyfunctionality in French deverbal nominalizations
AbstractThis article investigates the semantic polyfunctionality of affixes, i.e. their ability to serve a variety of distinct semantic functions. Based on the analysis of a sample of 3,091 deverbal nouns ending with 46 different suffixes in French, the study examines the diversity of semantic functions realized by deverbal suffixes, the distribution ...
Justine Salvadori, Richard Huyghe
openaire +2 more sources

