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Functionalizing Thiosemicarbazones for Covalent Conjugation [PDF]

open access: yesMolecules
Thiosemicarbazones (TSCs) with their modular character (thiosemicarbazides + carbonyl compound) allow broad variation of up to four substituents on the main R1R2C=N(1)–NH–C(S)–N(4)R3R4 core and are thus interesting tools for the formation of conjugates ...
Johannes Hohnsen   +5 more
doaj   +4 more sources

Evolution of Thiosemicarbazones: From First- to Second-Generation Metal Chelators and Their Reactive Oxygen Species-Mediated Effects in Melanoma. [PDF]

open access: yesChemistryOpen
Thiosemicarbazones (TSC) have demonstrated promise as new chemotherapeutic agents against melanoma in both in vitro and In vivo studies. TSC are powerful metal coordinating agents, coordinating transition metal ions such as zinc, copper and iron in multiple oxidation states. It is this metal coordination that imparts the anticancer activity.
Alim R, Andrew SD, Parkinson CJ.
europepmc   +2 more sources

In Silico Studies and Biological Evaluation of Thiosemicarbazones as Cruzain-Targeting Trypanocidal Agents for Chagas Disease [PDF]

open access: yesPharmaceutics
Background/Objectives: Chagas disease remains a major unmet medical need due to the limited efficacy and safety of current therapies. Here, we investigated sixteen thiosemicarbazone (TSC) derivatives as cruzain inhibitors using an integrated in silico/in
Lidiane Meier   +11 more
doaj   +2 more sources

Investigating Metal and Fluorophore Controlled Intracellular Localization in Noble Metal Thiosemicarbazone Complexes. [PDF]

open access: yesChemistry
Same ligand, same dye, different metal: Thiosemicarbazone conjugates of Pt and Pd show distinctly different localization patterns inside mammalian cells. Abstract Transition metal complexes have been widely utilized as cellular imaging tools. To impart organelle specificity, ligand architecture is usually modified to modulate properties like overall ...
Sheernaly N   +10 more
europepmc   +2 more sources

Design, synthesis, in vitro and in silico studies of novel piperidine derived thiosemicarbazones as inhibitors of dihydrofolate reductase [PDF]

open access: yesScientific Reports
Dihydrofolate reductase (DHFR), an essential enzyme in folate metabolism, presents a promising target for drug development against various diseases, including cancer and tuberculosis.
Hina Aftab   +9 more
doaj   +2 more sources

Synthesis, characterization and biological activity of Pt(II) complexes with steroidal thiosemicarbazones [PDF]

open access: yesJournal of the Serbian Chemical Society, 2021
In this work, Pt(II) complexes of previously synthesized steroidal thiosemicarbazones were synthesized and characterized. The ligands and their metal complexes were studied by analytical and spectroscopic data (elemental analysis, IR, 1D-NMR and 2D-NMR ...
Čobeljić Božidar R.   +6 more
doaj   +1 more source

Synthesis and Antioxidant Activity of Novel Thiazole and Thiazolidinone Derivatives with Phenolic Fragments

open access: yesApplied Sciences, 2023
In this work, a series of thiosemicarbazones with phenol fragments were used as starting compounds for the synthesis of new effective antioxidants containing both a phenol substituent and a heterocyclic fragment: thiazole and thiazolidinone. To determine
Vladimir N. Koshelev   +4 more
doaj   +1 more source

Synthesis of New of 4-Thiazolidinone and Thiazole Derivatives Containing Coumarin Moiety with Antimicrobial Activity

open access: yesActa Chimica Slovenica, 2023
Synthesizing hybrid molecules is one the best manner to achieve novel promising agents. Consequently, series of new thiazoles having coumarin nucleus were synthesized from 3-acetylcoumarin thiosemicarbazones. Cyclization of thiosemicarbazone derivatives
Reem Al-Harbi   +2 more
doaj   +1 more source

Trigonal-bipyramidal vs. octahedral coordination in indium(III) complexes with potentially S,N,S‐tridentate thiosemicarbazones [PDF]

open access: yes, 2020
Three bis‐chelates of indium(III) with (partially fluorinated) S,N,S‐tridentate thiosemicarbazones (H2L) were prepared and their structures were studied in solution and in the solid state by NMR, ESI MS and single‐crystal X‐ray diffraction.
Abram, Ulrich   +3 more
core   +1 more source

Monosubstituted Acetophenone Thiosemicarbazones as Potent Inhibitors of Tyrosinase: Synthesis, Inhibitory Studies, and Molecular Docking

open access: yesPharmaceuticals, 2021
A set of 12 monosubstituted acetophenone thiosemicarbazone derivatives (TSCs) were synthesized and their inhibitory properties toward tyrosinase activity were tested.
Katarzyna Hałdys   +4 more
doaj   +1 more source

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