N,N'-[4,4'-(perfluoro-1,4-phenylenedioxy)-bis(4,1-phenylene)]-bis[2-(pyridine-2-ilmethylene)hydrazinecarbothioamide] and use thereof as prostate cancer LNCaP cell proliferation inhibitor
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 procee...
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Zusammenfassung: | 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.
Invenţia se referă la chimia organică, şi anume la sinteza compuşilor biologic activi din clasa tiosemicarbazonelor şi poate găsi aplicare în medicină la profilaxia şi tratarea cancerului prostatei.Esenţa invenţiei constă în aceea că a fost sintetizat un compus nou pornind de la 4,4'-(perfluoro-1,4-fenilendioxi)dianilină, care a fost supusă următorului şir de transformări: trecerea în bis-tiouree la interacţiunea cu dimetiltiouram; dezaminarea cu acid sulfuric în bis-izotiocianat; transformarea la hidrazinoliză în bis-tiosemicarbazida respectivă, care a fost în continuare condensată cu 2-formilpiridină. În final se obţine N,N'-¢4,4'-(perfluoro-1,4-fenilendioxi)-bis(4,1-fenilen)]-bis¢2-(piridin-2-ilmetilen)hidrazincarbotioamidă] cu formula:Bis-tiosemicarbazona obţinută posedă activitate anticancerigenă, care depăşeşte de 1,5 ori activitatea doxorubicinei.Rezultatul tehnic al invenţiei constă în extinderea arsenalului de inhibitori ai proliferării celulelor LNCaP ale cancerului prostatei. |
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