Molecular inhibitor of HL-60 cancer cells' proliferation based on 2-{[2-(prop-2-en-1-ylcarbamothioyl) hydrazinylidene]-methyl} pyridinium nitrate
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GULYA, Aurelian, GRAUR, Vasilii О., CAZANJI, Irina, TSAPKOV, Victor I., CHUMAKOV, Yurii, PETRENKO, Peter A.. Molecular inhibitor of HL-60 cancer cells' proliferation based on 2-{[2-(prop-2-en-1-ylcarbamothioyl) hydrazinylidene]-methyl} pyridinium nitrate. In: Achievements and perspectives of modern chemistry, 9-11 octombrie 2019, Chişinău. Chisinau, Republic of Moldova: Tipografia Academiei de Ştiinţe a Moldovei, 2019, p. 221. ISBN 978-9975-62-428-2.
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Achievements and perspectives of modern chemistry 2019
Conferința "International Conference "Achievements and perspectives of modern chemistry""
Chişinău, Moldova, 9-11 octombrie 2019

Molecular inhibitor of HL-60 cancer cells' proliferation based on 2-{[2-(prop-2-en-1-ylcarbamothioyl) hydrazinylidene]-methyl} pyridinium nitrate


Pag. 221-221

Gulya Aurelian1, Graur Vasilii О.1, Cazanji Irina1, Tsapkov Victor I.1, Chumakov Yurii2, Petrenko Peter A.2
 
1 Moldova State University,
2 Institute of Applied Physics
 
Disponibil în IBN: 11 noiembrie 2019


Rezumat

Cancer is a group of diseases commonly found in the world, being one of the main causes of mortality. Chemotherapy is often used for cancer treatment. Substances that are used to treat cancer have some shortcomings, including high toxicity and low selectivity. Many substances with antiproliferative properties have low solubility in aqueous solutions, which reduces the possibility of their application in medical practice. Thiosemicarbazone class of organic substances attracts constant scientific interest due to its anticancer activity. Therefore, the study of new derivatives of N4-substituted thiosemicarbazones, which exhibit selective anticancer activity and increased solubility in water, is of interest from both theoretically and practically points of wiew. The aim of this work is to find the conditions of synthesis and to determine the structure and antiproliferative properties of 2-{[2-(prop-2-en-1-ylcarbamothioyl)hydrazinylidene]methyl}pyridinium nitrate (HL*HNO3). HL*HNO3 was obtained by reaction between 2-formylpyridine, N4-allyl-3thiosemicarbazone (HL) and nitric acid. The structure and purity of HL*HNO3 were determined by 1H and 13C NMR spectroscopy. The NMR data correspond to these from the literature for compounds with the protonated pyridine nitrogen atom. The peaks of pyridinic hydrogen atoms have higher chemical shifts compared to the same hydrogen atoms in corresponding thiosemicarbazone HL. Single crystals of the HL*HNO3 were obtained by recrystallization from ethanol. Empirical formula C10H13N5O3S; space group P 21/C; cell lengths [Å]: a = 5,1190(5); b = 16,353(2), c = 15,968(2); cell angles: a = 90o, b = 90,081(9)o, y = 90o. The solubility of HL*HNO3 is 5.0 mg/mL (18 mM) that is 35 times higher than the solubility of initial thiosemicarbazone HL. The molar conductivity of the 10-3 mol/L solution of HL*HNO3 in water corresponds to an electrolyte of type 1:1. It was studied the antitumor activity of synthesized substances on human leukemia HL-60 cells. The obtained IC50 value for HL*HNO3 is 0.1 μmol/L, but the IC50 for the initial thiosemicarbazone HL is 0.38 μmol/L. Thus the obtained salt is 3.8 times more active than HL and also 2 times more active than doxorubicin that is used in medical practice.figuraFigure. Crystal structure of HL*HNO3