Comparison of metabolic pathways of different α-N-heterocyclic thiosemicarbazones
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چکیده
منابع مشابه
Comparison of metabolic pathways of different α-N-heterocyclic thiosemicarbazones
Clinical failure of novel drugs is often related to their rapid metabolism and excretion. This highlights the importance of elucidation of their pharmacokinetic profile already at the preclinical stage of drug development. Triapine, the most prominent representative of α-N-heterocyclic thiosemicarbazones, was investigated in more than 30 clinical phase I/II trials, but the results against solid...
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Background Blocking of DNA synthesis through inhibition of ribonucleotide reductase has been proposed to be the main mechanism of anti-neoplastic action for a-N-heterocyclic thiosemicarbazones. Currently the best-studied agent of this class of compounds is triapine (3-amino-2-carboxaldehyde thiosemicarbazone), which has been tested in several phase I and II clinical trials. We synthesized triap...
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This investigation involved the synthesis of metal complexes to test the hypothesis that structural changesand metal coordination in pyridine thiosemicarbazones affect cell growth and cell proliferation in vitro. Thiosemicarbazones are well known to possess antitumor, antiviral, antibacterial, antimalarial, and other activities. Extensive research has been carried out on aliphatic, aromatic, he...
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heteropoly acids (hpa) and their salts have advantages as catalysts which make them both economically and environmentally attractive, strong br?nsted acidity, exhibiting fast reversible multi-electron redox transformations under rather mild conditions, very high solubility in polar solvents, fairly high thermal stability in the solid states, and efficient oxidizing ability, so that they are imp...
15 صفحه اولStudies of the antineoplastic activity and metabolism of -(N)-heterocyclic carboxaldehyde thiosemicarbazones in dogs and mice.
SUMMARY The antineoplastic effects of a-(/V)-heterocyclic Carboxaldehyde thiosemicarbazones were studied in dogs with lymphosarcoma, and some of their metabolic features were studied in both mice and dogs. Significant regression (38 to 72%) of tumor masses occurred in dogs treated with i.v. doses of 2 to 6 mg of the sodium salt of 1-formylisoquinoline thiosemicarbazone per kg for a maximum of 5...
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ژورنال
عنوان ژورنال: Analytical and Bioanalytical Chemistry
سال: 2018
ISSN: 1618-2642,1618-2650
DOI: 10.1007/s00216-018-0889-x