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2015 Vol 13 # 2


Ethylene: the laws of chemistry have not yet been canceled

B.A. Kurchii

IEC, 9, Gagarina Str., Irpin, 08200, Ukraine

Summary. The aim of this report is to present the mechanisms of ethylene functioning in the living systems on the bases of fundamental laws of chemical reactions. A point of view herein described is based on the free radical mechanism of ethylene action.

Keywords: ethylene, free radicals, receptors, gene key, gene lock.

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Synthesis of 2[
14Ń]-3-propoxy-1.4-benzdiazepine-2-one for pharmacokinetic research

V.I. Pavlovsky, V.B. Larionov, I.P. Valivodz’

A.V. Bogatsky Physico-Chemical Institute, NAS of Ukraine
86, Lyustdorfska doroga, Odesa, 65080, Ukraine

Summary. The aim of the work was synthesis of 214C-7-bromo-5-(o-chlorophenyl)-3-propoxy-1.2-dihydro-3H-1.4-benzdiazepine-2-one (BD-007), determination of its radiological properties as well as the possibility of use in pharmacological studies (isolation and determination in biological samples). BD-007 isotope 14C labeling was made at «2» position of heteroring, which remains in molecule after most of metabolic transformations, using 114C-glycine (via condensation of corresponding benzophenone with glycine chloroanhydride hydrochloride and further reaction of halogen derivative of 1.4-benzdiazepine with n-propyl alcohol). Radiochromatographic purity of obtained 2[14Ń]-7-bromo-3-propoxy-5-(2-chlorophenyl)-1,3-dihydro[å][1,4]diazepine-2-one substance was 66 % and specific activity 2,68 µCu/mol (0,16 kBk/mol), that is sufficient for primary studies in pharmacokinetics and metabolism. In model experiments the quantity of subsequent extractions and extragent/sample volumes ratio for isolation of radioactivity with required accuracy level (90, 95 or 99 %) were calculated. The determined analytical properties (variation coefficient ωs, 3,33 %, relative error, ε, 9,53 %) allow using of this method in pharmacokinetic studies.

Keywords: 2[14Ń]-3-propoxy-1.4-benzdiazepine-2-one, izotope labeling, determination validation.

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Cytotoxicity of 1-benzyl-3-chloro-4-an³l³no-2,5-dihydropyrrole-2,5-dione derivatives

S.S. Tarnavskyi1, O.V. Ostrynska1, G.P. Volynets1, K.V. Kotsarenko1,
Yu.A. Starosyla
2, M.V. Protopopov1, V.G. Bdzhola1, S.M. Yarmoluk1

1 Institute of Molecular Biology and Genetics, NAS of Ukraine
150, Zabolotnoho Str., Kyiv, 03680, Ukraine

2 National Technical University of Ukraine «Kyiv Polytechnic Institute»
37, Peremohy Ave., Kyiv, 03056, Ukraine

Summary. Twenty derivatives of the 1-benzyl-3-chloro-4-anilino-2,5-dihydro-1H-2,5-piroldion with different substituents at aniline and benzene rings were synthesized and tested for cytotoxic activity. Compounds were tested on cancer cell lines HCT-15, MSF7, Hs683, U-373MG, LoVo and A549. Five compounds were shown to inhibit the proliferation of cancer cells with IC50>5õ10-6 M.

Keywords: 1-benzyl-3-chloro-4-an³l³no-2,5-dihydro-1H-2,5-p³rold³on, MTT test, antitumoractivity.

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Search of new inhibitors of protein kinase CK2 among 2-pyridone derivatives

O.V. Ostrynska1, I.V. Ukrainets2, L.V. Sidorenko2, Yu.A. Starosyla3, M.V. Protopopov1, O.P. Kukharenko1, V.G. Bdzhola1, S.M. Yarmoluk1

1 Institute of Molecular Biology and Genetics, NAS of Ukraine
150, Zabolotnoho Str., Kyiv, 03680, Ukraine

2 National University of Pharmacy
53, Pushkinska Str., Kharkiv, 61002, Ukraine

3 National Technical University of Ukraine «Kyiv Polytechnic Institute»
37, Peremohy Ave., Kyiv, 03056, Ukraine

Summary. The search of inhibitors of protein kinase CK2 among 2-pyridone derivatives via receptor-based virtual screening and biochemical tests in vitro was carried out. It was found that one inhibitor from 15 selected compoundshave IC50=8.3 µM. The binding mode of this ligand with amino acid residue of ATP-acceptor site of protein kinase CK2 has been proposed.

Keywords: 2-pyridone, inhibitor of human protein kinase CK2, virtual screening.

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Synthesis and antitumor activity of 2-acetamido-5-benzylthiazol-4-yl acetates

B.D. Grishchuk1, R.V. Symchak1, V.S. Baranovskyi1, V.M. Yatsiuk1, V.S. Brovarets2

1 Ternopil V. Hnatiuk National Pedagogical University
2, M. Kryvonosa Str., Ternopil, 46027, Ukraine

2 Institute of Bioorganic and Petroleum Chemistry, NAS of Ukraine
1, Murmanska Str., Kyiv, 02094, Ukraine

Summary. 2-Acetamido-5-benzylthiazole-4-yl acetates were synthesized by cyclization of 3-aryl-2- thiocyanatopropanamides. Antitumor activity of these compounds on 60 lines of cancer cells was investigated. The synthesized compounds have displayed a moderate effect on the line of renal cancer A498 and CNS cancer SNB-75.

Keywords: 2-aminothiazole, anionarylation, 2-acetamido-5-benzylthiazol-4-yl acetates, antitumor activity.

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