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2005 Vol II #1



Design of multi-channel fluorescent probes on the basis of 3-hydroxychromones
and their analogues


V. H. Pyvovarenko

Department of Chemistry, Taras Shevchenko National University
64 Volodymyrska Str., Kyiv, 01033, Ukraine

Abstract: The design of multi-channel fluorescent probes for the study of physical parameters of homogeneous and heterogeneous liquid media are discussed. The review deals with the design, synthesis luminescence and sensor properties in organic solvents, micelles and liposomes of multi-channel probes on the basis of 3-hydroxychromones as well as cation indicators on this basis.

Key words: fluorescent probes, fluorescent sensors, excited state intramolecular proton transfer, 3-hydroxy-
chromones, 3-hydroxyflavones, flavonols, diflavonols.

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Side reactions of onium coupling reagents BOP and HBTU in the synthesis of silica polymer supports


L. V. Dubey, I. Ya. Dubey

Institute of Molecular Biology and Genetics,
NAS of Ukraine
150 Zabolotnogo str., 03143, Kyiv, Ukraine


Abstract: Onium activating reagents BOP and HBTU have been used for the polymer linker elongation via the coupling of COOH function with amino group. Possible side reactions accompanying linker synthesis in the presence of BOP and HBTU and their effect on the coupling yields have been studied in model experiments. The results demonstrate that BOP is more stable in the reaction medium than HBTU, with equal coupling efficiency in regular condensation reactions. HBTU can react with amino polymer decreasing coupling yield, whereas it is not the case for BOP. It is thus recommended to avoid the interaction of HBTU reagent with amino polymer before the addition of carboxylic component. Short preactivation of the amino acid component with onium reagents increases the yield of subsequent coupling reaction.

Key words: polymer supports, coupling reagents, phosphonium salts, uronium salts, side reactions.

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C
omparative analysis of the similarity between primary sequences of receptor CD4 and protein kinases


Yu. Ya. Kit

Institute of Cell Biology, NAS of Ukraine
14/16 Dragomanov Str., 79005, Lviv, Ukraine


Abstract: The protein kinase activity of a recombinant extracellular fragment of the CD4 receptor (rsCD4) has been demonstrated earlier. The catalytic domain of this protein is not yet known. Using the library of amino acid sequences of different protein kinases (KinBase) and the search program Kinom Blast Server the author has realized the investigation of homology levels between the CD4 and other known protein kinases. The comparative analysis carried out shows the CD4 to contain a sequence highly similar to some motifs of calcium/calmodu-lin-regulated kinases; it is located on the N-terminal part of the rsCD4 molecule. This sequence consists of ca. 150 amino acids and includes an IgV region and the main part of the first Ig-like domain of CD4. The phosphorylation site common for the protein kinase C family has been also detected within this sequence. We suggest it participates in the formation of the CD4 catalytic domain.

Key words: CD4 receptor, protein kinases, comparative analysis.

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I
nfluence of a tetranucleotide, CGCG, on marine algal viruses


O. A. Stepanova

Alexander O. Kovalevsky Institute of Biology of Southern Seas, NAS of Ukraine
2 Nakhimov avenue, Sevastopol, 99011, Ukraine

Abstract: The author shows a tetranucleotide, CGCG, to inhibit infectious activities of some algal viruses by 102104 times. This process depends on the duration of CGCG-virus contact. The results obtained seem to be interesting from the practical point of view.

Key words: CGCG, algal viruses, infectious activity.

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This article is sponsored by Otava, Ltd.

Search for protein kinase CK2 inhibitors among 3-carboxy-4-aminoquinoline derivatives


V. M. Sapelkin, A. G. Golub, O. Ya. Yakovenko,
V. G. Bdzhola, S. M. Yarmoluk

Institute of Molecular Biology and Genetics,
NAS of Ukraine
150 Zabolotny Str., Kyiv-143, 03143, Ukraine

Abstract: 52 compounds from combinatorial library of 4-amino-3-carbethoxy-quinoline derivatives have been chosen using receptor-based virtual screening technology for studying their CK2 inhibition activity. It has been shown that 6 substances inhibit CK2 activity by more than 70 %. IC50 of these compounds ranged from 9 to 19 μM. The most potent inhibitor, 1.32 (3,6-dicarbethoxy-4-(4-acetamidophenylamino)quinoline, has IC50 9 μM. Model of binding of 4-amino-3-carbethoxy-quinoline derivatives to ATP-site of CK2 and structure-activity relationship are also proposed.

Key words: CK2 inhibitors, 4-amino-3-carbethoxy-quinoline derivatives, receptor based virtual screening.

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This article is sponsored by Otava, Ltd.

Synthesis of 7-(3-dialkylamino-2-hydroxypropoxy)-3-aryloxychromones

A. O. Prykhodko, S. P. Kobzev1, S. M. Yarmoluk

Institute of Molecular Biology and Genetics,
NAS of Ukraine
150 Zabolotny Str., Kyiv, 03143, Ukraine

1L.M. Litvinenko Institute of Physical-Organic Chemistry and Coal Chemistry, NAS of Ukraine
70 R. Luxemburg Str., Donetsk, 83114, Ukraine

Abstract: By reaction of alkilation 3-aryloxychromones with epichlorohydrin were obtained 7-epoxyderivatives, which reacted with secondary amines to give the derivatives of 3-dialkylamino-2-hydroxypropane.

Key words: 3-aryloxychromone, oxiranylmethoxy, 3-dial-
kylamino-2-hydroxypropane.

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