首页> 外国专利> N,N'-4,4'-(perfluoro-1,4-phenylenedioxy)-bis(4,1-phenylene)-bis2-(pyridine-2-ilmethylene)hydrazinecarbothioamide and use thereof as prostate cancer LNCaP cell proliferation inhibitor

N,N'-4,4'-(perfluoro-1,4-phenylenedioxy)-bis(4,1-phenylene)-bis2-(pyridine-2-ilmethylene)hydrazinecarbothioamide and use thereof as prostate cancer LNCaP cell proliferation inhibitor

机译:N,N'-[4,4'-(全氟-1,4-苯二氧基)-双(4,1-亚苯基)]-双[2-(吡啶-2-基亚甲基)肼基碳硫代酰胺]及其作为前列腺癌的用途LNCaP细胞增殖抑制剂

摘要

The invention relates to organic chemistry, namely to the synthesis of biologically active compounds from the class of thiosemicarbazones and can be used in medicine for the prevention and treatment of prostate cancer.Summary of the invention consists in that it was synthesized a new compound proceeding from 4,4'-(perfluoro-1,4-phenylenedioxy)dianiline, which was subjected to the following series of transformations: conversion into bis-thiourea upon interaction with dimethylthiouram; deamination with sulfuric acid in bis-isothiocyanate; conversion upon hydrazinolysis into appropriate bis-thiosemicarbazide, which was further condensed with 2-formylpyridine. Finally, it is obtained N,N'-[4,4'-(perfluoro-1,4-phenylenedioxy)-bis(4,1-phenylene)]-bis[2-(pyridine-2-ilmethylene) hydrazinecarbothioamide] with the formula:The resulting bis-thiosemicarbazone possesses anticancer activity, which 1.5 times exceeds the activity of doxorubicine.The technical result of the invention is to expand the range of prostate cancer LNCaP cell proliferation inhibitors.
机译:本发明涉及有机化学,即涉及一种由硫代半氨基甲酮类生物活性化合物的合成,可用于预防和治疗前列腺癌的药物。 4,4'-(全氟-1,4-苯二氧基)二苯胺,经过以下一系列的转化反应:与二甲基硫氧嘧啶相互作用转化为双硫脲;在双异硫氰酸酯中用硫酸脱氨基;在肼解后转化为合适的双-硫代氨基脲,将其进一步与2-甲酰基吡啶缩合。最终,得到N,N′-[4,4′-(全氟-1,4-苯二氧基)-双(4,1-亚苯基)]-双[2-(吡啶-2-基亚甲基)肼基甲硫基酰胺]。分子式:所得到的双硫半脲具有抗癌活性,是阿霉素活性的1.5倍。本发明的技术成果是扩大前列腺癌LNCaP细胞增殖抑制剂的范围。

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