Results 1 to 10 of about 2,278 (177)

Functionalizing Thiosemicarbazones for Covalent Conjugation [PDF]

Molecules
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, Lukas Rryci, Diana Obretenova, Joshua Friedel, Shahab Jouchaghani, Axel Klein   +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]

ChemistryOpen
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

Cruzain Inhibitors for Chagas Disease: Anticorrelated Optimisation Landscapes and the Multiparametric Path to Clinical Candidates. [PDF]

Chem Biol Drug Des
Three decades of cruzain‐targeted drug discovery have yielded 215 sub‐micromolar inhibitors but no clinical candidates. This review diagnoses a systemic translational failure driven by single‐parameter optimisation and proposes a multiparametric framework integrating enzymatic potency, cathepsin selectivity, intracellular exposure, and metabolic ...
Dos Reis CRC, de Souza HVCM, Parra LC, de Souza GVCM, Zorzanelli BC, Boechat N, Hoelz LVB, Fernandes TVA.   +7 more
europepmc   +2 more sources

Monoamine Oxidase and Cholinesterase Inhibition Profiles of Semicarbazone and Thiosemicarbazone Derivatives. [PDF]

Chem Biodivers
Thiosemicarbazones generally show higher MAO‐B inhibitory potential than their corresponding semicarbazones, and particularly T6 is the most potent, which contains R = H and X = S in its Tail Unit, with an IC50 value of 6.45 µM with SI of 3.6. ABSTRACT Twenty semicarbazone and thiosemicarbazone derivatives (T1–T20) were synthesized and evaluated for ...
Bindra S, Jeong WK, Kabier M, Kumar S, Sudevan ST, Vishwakarma HC, Parambi DGT, Maliyakkal N, Kumar S, Pappachen LK, Kim H, Mathew B.   +11 more
europepmc   +2 more sources

From Design to Bioactivity: 2-Benzoylpyridine 4-(bicyclo[2.2.1]hept-2-yl)thiosemicarbazone and Its 3d Metal Coordination Compounds. [PDF]

ChemistryOpen
The new 2‐benzoylpyridine 4‐(bicyclo[2.2.1]hept‐2‐yl)thiosemicarbazone (HL) and its copper(II), nickel(II), cobalt(III), and iron(III) coordination compounds [Cu(L)Cl] (1), [Cu(L)NO3] (2), {[Cu(L)(Cl2CHCOO)]}n (3), [Ni(HL)2](NO3)2 (4), [Fe(L)2]NO3 (5), [Co(L)2]NO3 (6) were obtained.
Graur I, Graur V, Melnic E, Lozan-Tirsu C, Balan G, Tsapkov V, Gulea A.   +6 more
europepmc   +2 more sources

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

Pharmaceutics
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, Milena F. C. V. de Melo, Heitor R. Abreu, Isabella M. e Oliveira, Larissa Sens, Thiago H. Doring, Renata Krogh, Adilson Beatriz, Adriano D. Andricopulo, Sumbal Saba, Aldo S. de Oliveira, Jamal Rafique   +11 more
doaj   +2 more sources

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

Journal 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., Živković Marijana B., Matić Ivana Z., Novaković Irena T., Sladić Dušan M., Anđelković Katarina K., Krstić Natalija M.   +6 more
doaj   +1 more source

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

Scientific 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, Saeed Ullah, Ajmal Khan, Mariya al-Rashida, Talha Islam, Kholood A. Dahlous, Saikh Mohammad, Hamdy Kashtoh, Ahmed Al-Harrasi, Zahid Shafiq   +9 more
doaj   +2 more sources

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

Applied 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, Olga V. Primerova, Stepan V. Vorobyev, Anna S. Stupnikova, Ludmila V. Ivanova   +4 more
doaj   +1 more source

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

Acta 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, Marwa El-Sharief, Samir Abbas   +2 more
doaj   +1 more source