thiourea and thiocarbohydrazide

A new series of isatin-β-thiocarbohydrazones was synthesized based on the pharmacophoric features of triapine required for metal chelation. Our strategy involved the modifications of triapine basic skeleton by replacing pyridinyl moiety with isatin which retains the tridentate feature of triapine needed for metal chelation. The new compounds were esteemed for their antitumor efficacy against cervical cancer (Hela) and kidney fibroblast cancer (COS-7) cell lines. Compounds 4c, 4d, 5c and 5e exhibited remarkable efficacy against Hela cell line. In addition, compounds 4c, 4k, 4e, 5c and 5e displayed an outstanding efficacy against COS-7 cell line. Compounds 4c, 4k, 4e, 5c and 5e were examined for their in vivo antitumor efficacy against Ehrlich ascites carcinoma (EAC) in mice. Pharmacophore mapping was performed to study the structural features of the synthesized compounds compared to triapine and to identify the essential moieties required for potent and selective antitumor activity.

Topics: Animals; Antineoplastic Agents; Apoptosis; Carcinoma, Ehrlich Tumor; Cell Proliferation; Chlorocebus aethiops; COS Cells; Drug Screening Assays, Antitumor; HeLa Cells; Humans; Hydrazines; Indoles; Isatin; Male; Mice; Microwaves; Structure-Activity Relationship; Thiourea

By a simple and convenient method of using formaldehyde as linkages, two new chitosan (CS) derivatives modified respectively with thiosemicarbazide (TSFCS) and thiocarbohydrazide (TCFCS) were synthesized. The new compounds were characterized and studied by Fourier transform infrared spectroscopy, elemental analysis, thermal gravity analysis and differential scanning calorimetry, and their surface morphologies were determined via scanning electron microscopy. These CS derivatives could form pH dependent gels. The behavior of 304 steel in 2% acetic acid containing different inhibitors or different concentrations of inhibitor had been studied by potentiodynamic polarization test. The preliminary results show that the new compound TCFCS can act as a mixed-type metal anticorrosion inhibitor in some extent; its inhibition efficiency is 92% when the concentration was 60 mg/L. The adsorption studies on a metal ion mixture aqueous solution show that two samples TSFCS and TCFCS can absorb As (V), Ni (II), Cu (II), Cd (II) and Pb (II) efficiently at pH 9 and 4.

Topics: Adsorption; Amines; Chitosan; Corrosion; Electrochemical Techniques; Hydrazines; Hydrogen-Ion Concentration; Metals, Heavy; Microscopy, Electron, Scanning; Nanoparticles; Semicarbazides; Spectroscopy, Fourier Transform Infrared; Surface Properties; Thiourea