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Semicarbazones and thiosemicarbazones: their wide pharmacological profile and clinical applications

机译:半咔唑酮和硫代半咔唑酮:它们的广泛药理特性和临床应用

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This article shows that thiosemicarbazones, semicarbazones and their metal complexes can exhibit target selectivity along with a wide pharmacological profile. Complexes of thiosemicarbazones with cytotoxic or antitumoral activity are presented, some of which show activity against cisplatinum-resistant cells. The inhibition mechanism of the enzyme ribonucleoside diphosphate reductase (RDR), involved in DNA syntheses, by a(N)-heterocyclic thiosemicarbazones is discussed. The encouraging results of clinical trials with the RDR inhibitor 3-aminopyridine-2-carboxaldehyde thiosemicarbazone ("Triapine") against rapidly growing tumors are outlined. Examples are also given of thiosemicarbazones with antiviral and antimicrobial activity. The possible applications of semicarbazones as anticonvulsants with low toxicity and good therapeutic index are presented.
机译:本文表明,硫代半咔唑酮,半咔唑酮及其金属配合物可以表现出目标选择性以及广泛的药理作用。提出了具有细胞毒性或抗肿瘤活性的硫半脲化合物,其中一些对顺铂耐药细胞具有活性。讨论了核糖核苷酸核苷二磷酸还原酶(RDR)参与DNA合成的α(N)-杂环硫代半氨基咔唑酮的抑制机理。概述了使用RDR抑制剂3-氨基吡啶-2-羧甲醛硫代半碳酸盐(“三氮平”)针对快速生长的肿瘤的令人鼓舞的临床试验结果。还给出了具有抗病毒和抗微生物活性的硫代半咔唑的实例。提出了氨基脲作为低毒性和良好治疗指数的抗惊厥药的可能应用。

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