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Thiosemicarbazones as Potent Anticancer Agents and their Modes of Action.
Mini-Reviews in Medicinal Chemistry ( IF 3.8 ) Pub Date : 2020-01-01 , DOI: 10.2174/1389557519666191029130310
Bhushan Shakya 1 , Paras Nath Yadav 2
Affiliation  

Thiosemicarbazones (TSCs) are a class of Schiff bases usually obtained by the condensation of thiosemicarbazide with a suitable aldehyde or ketone. TSCs have been the focus of chemists and biologists due to their wide range of pharmacological effects. One of the promising areas in which these excellent metal chelators are being developed is their use against cancer. TSCs have a wide clinical antitumor spectrum with efficacy in various tumor types such as leukemia, pancreatic cancer, breast cancer, non-small cell lung cancer, cervical cancer, prostate cancer and bladder cancer. To obtain better activity, different series of TSCs have been developed by modifying the heteroaromatic system in their molecules. These compounds possessed significant antineoplastic activity when the carbonyl attachment of the side chain was located at a position α to the ring nitrogen atom, whereas attachment of the side chain β or γ to the heterocyclic N atom resulted in inactive antitumor agents. In addition, replacement of the heterocyclic ring N with C also resulted in a biologically inactive compound suggesting that a conjugated N,N,S-tridentate donor set is essential for the biological activities of thiosemicarbazones. Several possible mechanisms have been implemented for the anticancer activity of thiosemicarbazones.

中文翻译:

硫代氨基脲类作为有效的抗癌剂及其作用方式。

硫代氨基咔唑(TSC)是一类席夫碱,通常通过将硫代氨基脲与合适的醛或酮缩合而获得。由于TSC具有广泛的药理作用,因此一直是化学家和生物学家关注的焦点。这些优异的金属螯合剂正在开发中的有前途的领域之一是它们对癌症的用途。TSC具有广泛的临床抗肿瘤谱,可有效治疗多种肿瘤,例如白血病,胰腺癌,乳腺癌,非小细胞肺癌,宫颈癌,前列腺癌和膀胱癌。为了获得更好的活性,已经通过修饰分子中的杂芳族体系开发了不同系列的TSC。当侧链的羰基连接位于环氮原子的位置α时,这些化合物具有显着的抗肿瘤活性,而侧链β或γ与杂环N原子的连接导致抗肿瘤剂失活。另外,用C取代杂环N也导致生物惰性的化合物,这表明共轭的N,N,S-三齿供体对硫代半氨基甲酮的生物活性是必不可少的。已为硫代半氨基甲酮类药物的抗癌活性实施了几种可能的机制。用C取代杂环N还会产生生物惰性的化合物,这表明共轭的N,N,S-三齿供体对硫代半氨基甲酮的生物活性至关重要。已为硫代半氨基甲酮类药物的抗癌活性实施了几种可能的机制。用C取代杂环N还会产生生物惰性的化合物,这表明共轭的N,N,S-三齿供体对硫代半氨基甲酮的生物活性至关重要。已为硫代半氨基甲酮类药物的抗癌活性实施了几种可能的机制。
更新日期:2019-11-01
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