Photoswitchable Azo- and Diazocine-Functionalized Derivatives of the VEGFR-2 Inhibitor Axitinib. [PDF]
In this study, we aimed at the application of the concept of photopharmacology to the approved vascular endothelial growth factor receptor (VEGFR)-2 kinase inhibitor axitinib.
Heintze L +7 more
europepmc +5 more sources
Unsymmetrically Substituted Dibenzo[b,f][1,5]-diazocine-6,12(5H,11H)dione—A Convenient Scaffold for Bioactive Molecule Design [PDF]
A novel approach for the synthesis of unsymmetrically substituted dibenzo[b,f][1,5]diazocine-6,12(5H,11H)diones has been developed. This facile three-step method uses variously substituted 1H-benzo[d][1,3]oxazine-2,4-diones (isatoic anhydrides) and 2 ...
Bartosz Bieszczad +6 more
doaj +3 more sources
Synthesis and Spectral Characterization of Benzo-[6,7][1,5]diazocino[2,1-a]isoindol-12-(14H)-one Derivatives [PDF]
A simple synthetic route affording 27%–85% yields of benzo[6,7][1,5]diazocino[2,1-a]isoindol-12(14H)-one ring systems from readily available 3-(2-oxo-2-phenylethyl) isobenzofuran-1(3H)-ones and 2-(aminomethyl)aniline starting materials in toluene and ...
Jatinder P. Bassin +5 more
doaj +4 more sources
Improved HDAC Inhibition, Stronger Cytotoxic Effect and Higher Selectivity against Leukemias and Lymphomas of Novel, Tricyclic Vorinostat Analogues [PDF]
Histone deacetylase (HDAC) inhibitors are a class of drugs used in the cancer treatment. Here, we developed a library of 19 analogues of Vorinostat, an HDAC inhibitor used in lymphomas treatment.
Bartosz Bieszczad +7 more
doaj +2 more sources
Facile Synthesis of Light-Switchable Polymers with Diazocine Units in the Main Chain. [PDF]
Li S +4 more
europepmc +2 more sources
Light-Driven Ratchet Mechanism Accelerates Regioselective Metal-Cation Exchange in a Heterobimetallic Helicate. [PDF]
Photoswitchable homo‐ and heterobimetallic helicates form with high diastereo‐ and regioselectivity via single‐step self‐assembly or self‐sorting. White‐light exposure autonomously operates one helicate as a molecular ratchet, promoting the selective formation of an out‐of‐equilibrium structure.
Notheis MJ +2 more
europepmc +3 more sources
Comparative studies of the Pschorr reaction in the pyrazole series. Access to the new dibenzo[e,g]pyrazolo[1,5-a][1,3]diazocine system of pharmaceutical interest [PDF]
The diazonium tetrafluoroborate 11 obtained from 2-amino-N-methyl-N-(1-phenyl-3-methylpyrazol-5-yl)benzamide was transformed in dry acetonitrile via an ionic or radical pathway. Diferences were observed with respect to ionic or radical transformations in
Benedetta Maggio +8 more
doaj +3 more sources
Light-Controlled Destruction and Assembly: Switching between Two Differently Composed Cage-Type Complexes. [PDF]
We report on two regioisomeric, diazocine ligands 1 and 2 that can both be photoswitched between the E- and Z-configurations with violet and green light.
Hugenbusch D +4 more
europepmc +3 more sources
Real-Time In Situ Imaging of Aggregation-Induced Emission and Solvent-Guided Morphogenesis of a "V-Shaped" 4-Amino-1,8-Naphthalimide Tröger's Base Supramolecular Scaffold. [PDF]
It is demonstrated that the self‐assembly process of the 3‐pyridyl‐based TBNap structure is highly solvent deepened. X‐ray diffraction analysis confirms that the TBNap structure possesses solvent‐depended packing arrangements in the crystalized form.
Shanmugaraju S +6 more
europepmc +2 more sources
Photoswitchable Diazocine Derivative for Adenosine A<sub>3</sub> Receptor Activation in Psoriasis. [PDF]
Altres ajuts: CERCA Programme/Generalitat de CatalunyaIncorporating photoisomerizable moieties within drugs offers the possibility of rapid and reversible light-dependent switching between active and inactive configurations.
López-Cano M +11 more
europepmc +5 more sources

