MD4126C1 - N,N'-[4,4'-(perfluoro-1,4-fenilendioxi)-bis(4,1-fenilen)]-bis[2-(piridin-2-ilmetilen)hidrazincarbotioamidă] şi utilizarea ei în calitate de inhibitor al proliferării celulelor LNCaP ale cancerului prostatei - Google Patents

N,N'-[4,4'-(perfluoro-1,4-fenilendioxi)-bis(4,1-fenilen)]-bis[2-(piridin-2-ilmetilen)hidrazincarbotioamidă] şi utilizarea ei în calitate de inhibitor al proliferării celulelor LNCaP ale cancerului prostatei

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Publication number
MD4126C1
MD4126C1 MDA20100129A MD20100129A MD4126C1 MD 4126 C1 MD4126 C1 MD 4126C1 MD A20100129 A MDA20100129 A MD A20100129A MD 20100129 A MD20100129 A MD 20100129A MD 4126 C1 MD4126 C1 MD 4126C1
Authority
MD
Moldova
Prior art keywords
bis
phenylenedioxy
perfluoro
prostate cancer
ilmethylene
Prior art date
Application number
MDA20100129A
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English (en)
Russian (ru)
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MD4126B1 (ro
Inventor
Аурелиан ГУЛЯ
Анжела ЖАЛБЭ
Никанор БАРБА
Виктор ЦАПКОВ
Лариса СОФРОНИ
Дональд ПОЙРИЕР
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Государственный Университет Молд0
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Государственный Университет Молд0 filed Critical Государственный Университет Молд0
Priority to MDA20100129A priority Critical patent/MD4126C1/ro
Publication of MD4126B1 publication Critical patent/MD4126B1/ro
Publication of MD4126C1 publication Critical patent/MD4126C1/ro

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

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.
MDA20100129A 2010-11-15 2010-11-15 N,N'-[4,4'-(perfluoro-1,4-fenilendioxi)-bis(4,1-fenilen)]-bis[2-(piridin-2-ilmetilen)hidrazincarbotioamidă] şi utilizarea ei în calitate de inhibitor al proliferării celulelor LNCaP ale cancerului prostatei MD4126C1 (ro)

Priority Applications (1)

Application Number Priority Date Filing Date Title
MDA20100129A MD4126C1 (ro) 2010-11-15 2010-11-15 N,N'-[4,4'-(perfluoro-1,4-fenilendioxi)-bis(4,1-fenilen)]-bis[2-(piridin-2-ilmetilen)hidrazincarbotioamidă] şi utilizarea ei în calitate de inhibitor al proliferării celulelor LNCaP ale cancerului prostatei

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
MDA20100129A MD4126C1 (ro) 2010-11-15 2010-11-15 N,N'-[4,4'-(perfluoro-1,4-fenilendioxi)-bis(4,1-fenilen)]-bis[2-(piridin-2-ilmetilen)hidrazincarbotioamidă] şi utilizarea ei în calitate de inhibitor al proliferării celulelor LNCaP ale cancerului prostatei

Publications (2)

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MD4126B1 MD4126B1 (ro) 2011-09-30
MD4126C1 true MD4126C1 (ro) 2012-04-30

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MDA20100129A MD4126C1 (ro) 2010-11-15 2010-11-15 N,N'-[4,4'-(perfluoro-1,4-fenilendioxi)-bis(4,1-fenilen)]-bis[2-(piridin-2-ilmetilen)hidrazincarbotioamidă] şi utilizarea ei în calitate de inhibitor al proliferării celulelor LNCaP ale cancerului prostatei

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Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MD4215C1 (ro) * 2012-07-09 2013-11-30 Государственный Университет Молд0 Inhibitor al leucemiei mieloide umane în bază de N-(4-(5-(piridin-2-il)-4,5-dihidro-1H-pirazol-3-il)fenil)-2-(piridin-2-ilmetilen)-hidrazincarbotioamidă

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MD3771G2 (ro) * 2008-04-30 2009-07-31 Государственный Университет Молд0 Inhibitori ai enzimei 17β-HSD, stimulatoare a multiplicării celulelor cancerului prostatei
MD3996C2 (ro) * 2009-05-25 2010-07-31 Государственный Университет Молд0 Percloraţi de 5-R-saliciliden-4-feniltiosemicarbazonato(1-)-aquacupru(II) ce posedă proprietăţi de inhibitori ai activităţii enzimei 17 b-HSD (tipul 1)

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JPS5242883A (en) * 1975-10-03 1977-04-04 Otou Kenkyusho Method of preparing thiosemicarbazones having carcinostatic activity
US5281715A (en) * 1992-05-13 1994-01-25 Yale University 2-formylpyridine thiosemicarbazone compounds
RU2198875C2 (ru) * 1997-05-15 2003-02-20 Вион Фармасьютикалз, Инк. Способы получения тиосемикарбазонов пиридин-2-карбоксальдегидов и промежуточных пиридин-2-карбоксальдегидов
US5869676A (en) * 1997-05-15 1999-02-09 Vion Pharmaceuticals, Inc. Process for the synthesis of ribonucleotide reductase inhibitors 3-AP and 3-AMP
US5767134A (en) * 1997-05-15 1998-06-16 Vion Pharmaceuticals, Inc. Prodrug forms of ribonucleotide reductase inhibitors 3-AP and 3-AMP
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MD1274G2 (ro) * 1999-01-20 2000-02-29 Государственный Университет Молд0 Procedeu de obţinere a oligo-4-(4-tiosemicarbazido)stirenului
US6794400B2 (en) * 2001-06-01 2004-09-21 Cytovia, Inc. 4-substituted-1-(arylmethylidene)thiosemicarbazide, 4-substituted-1-(arylcarbonyl)thiosemicarbazide and analogs as activators of caspases and inducers of apoptosis and the use thereof
GB2392386A (en) * 2002-08-29 2004-03-03 Cxr Biosciences Ltd Medical use of perfluoro compounds
WO2007035489A2 (en) * 2005-09-16 2007-03-29 Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Methods of treating or preventing cancer using pyridine carboxaldehyde pyridine thiosemicarbazone radiosensitizing agents
MD3771G2 (ro) * 2008-04-30 2009-07-31 Государственный Университет Молд0 Inhibitori ai enzimei 17β-HSD, stimulatoare a multiplicării celulelor cancerului prostatei
MD3996C2 (ro) * 2009-05-25 2010-07-31 Государственный Университет Молд0 Percloraţi de 5-R-saliciliden-4-feniltiosemicarbazonato(1-)-aquacupru(II) ce posedă proprietăţi de inhibitori ai activităţii enzimei 17 b-HSD (tipul 1)

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Brockman R.W. et al: "Observations on the Antileukemic Activity of Pyridine-2-Carboxaldehyde Thiosemicarbazones and Thiocarbazone", Cancer Res. 1956 vol.16, p.167 *
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