[The synthesis of ψ-(2-aryl-1,3-dioxolan-2-yl) alkyl derivatives of purines and their activity towards HIV reverse transcriptase].

Novel non-competitive inhibitors of HIV RT were synthesized by alkylation of 6-substituted purines with different 2-(chloroalkyl)-2-aryl-1,3-dioxolanes and related compounds. The structure-activity relationship within the synthesized compounds was studied.

[The search of novel inhibitors of HIV-1 integrase among 5-(4-halogenophenyl)-5-oxopentyl derivatives of nucleic bases].

By alkylation of uracil, thymine, cytosine, adenine, 6-chloropurine, and 2-amino-6-chloropurine with 5-chloro-1-(4-halogenophenyl)-1-pentanones novel derivatives of nucleic bases were obtained, their physicochemical properties were studied. The influence of synthesized compounds on HIV-1 integrase was investigated.

[Polymethylene derivatives of nucleic bases bearing omega-functional groups. VIII. omega-oxo-omega-phenylalkyl pyrimidines and purines].

Novel polymethylene derivatives of nucleic bases containing a phenylketo function in the omega-position of hydrocarbon chain were synthesized by alkylation of uracil, thymine, cytosine, hypoxantine, adenine, and N(2)-isobutyrylguanine with omega-chloro-1 -phenylalkan-1-ones, their physicochemical properties were studied.

[The interaction of NS3 protein of hepatitis C virus with polymethylen derivatives of nucleic bases].

NS3 protein of hepatitis C virus plays the key role in the virus functioning. It possesses three enzymatic activities, namely protease activity, associated with N-terminal domain of the protein, and helicase/NTPase activities specific for C-terminal domain. Here, the effect of some polimethylenic derivatives of the nucleic bases on helicase and ATPase enzyme activities has been studied. Several of compounds tested displayed inhibitory activity towards NS3 helicase. However, most compounds demonstrated strong activating effect on ATPase activity of the enzyme as well as several other ATPases. The ATPase activating mechanism was not described earlier. The activation potency of the compounds depended on substrate/activator concentration ratio, and was maximal at the 1000:1. The activation mechanism scheme that allows us to explain phenomena observed is proposed.

[Polymethylene derivatives of nucleic bases with omega-functional groups: VII. Cytotoxicity in the series of N-(2-oxocyclohexyl)-omega-oxoalkyl substituted purines and pyrimidines].

New polymethylene derivatives of nucleic bases with a beta-diketo function in the omega-position were obtained by alkylation of uracil, thymine, cytosine, hypoxanthine, adenine, and N(2)-isobutyryl guanine with 2-omega-chloroal-kanoyl)cyclohexanones. The physical and chemical characteristics of the compounds synthesized and their effect on the K562 and HCT116 tumor cell lines were studied.

[Polymethylene nucleic acid derivatives with omega-functional groups: vi. [8-(2-oxocyclohexyl)-9-oxooctyl]pyrimidines as potential inhibitors of pyrimidine phosphorylases].

New polymethylene derivatives of nucleic bases with beta-diketo function in omega-position were prepared by alkylation of uracil, thymine, and cytosine. Their physicochemical properties and effect on the E. coli uridine phosphorylase were studied.

[Polymethylene derivatives of nucleic bases with omega-functional groups. V. Pyrimidine- and purine-containing gamma-butyrophenones].

New polymethylene derivatives of nucleic bases containing a keto function in the omega-position were synthesized by alkylation of nucleic bases with 2-(3-chloropropyl)-2-phenyl-1,3-dioxolane and the subsequent deblocking of the keto group; their physicochemical properties were studied. The English version of the paper: Russian Journal of Bioorganic Chemistry, 2005, vol. 31, no. 6; see also http://www.maik.ru.

[Polymethylene derivatives of nucleic bases with omega-functional groups: IV. [7-(2-oxocyclohexyl)-7-oxoheptyl]purines].

New polymethylene nucleoside analogues with a beta-dioxo function in the omega-position of their hydrocarbon chain, [7-(2-oxocyclohexyl)-7-oxoheptyl]purines, were synthesized, and their physicochemical properties were studied. The English version of the paper: Russian Journal of Bioorganic Chemistry, 2005, vol. 31, no. 3; see also http://www.maik.ru.

[Polymethylene derivatives of nucleic bases with omega-functional groups. III. N-[7-(2-oxocyclohexyl)-7-oxoheptyl]-substituted pyrimidines]. / Polimetilenovye proizvodnye nukleinovykh osnovanii s omega-funktsional'nymi gruppami. III. N-[7-(2-oksotsiklogeksil)-7-oksogeptil]-zameshennye pirimidiny.

New polymethylene derivatives of nucleic bases containing a beta-dioxo function at the omega-position were synthesized by alkylation of uracil, thymine, and cytosine with 1-(7-chloroheptanoyl)cyclohexan-2-one, and their physicochemical properties were studied. The English version of the paper: Russian Journal of Bioorganic Chemistry, 2004, vol. 30, no. 5; see also http: // www.maik.ru.

Thermal lens studies of the reaction of iron (II) with 1,10-phenanthroline at the nanogram level.

The determination of iron(II) with 1,10-phenanthroline in aqueous solutions was carried out exemplarily by thermal lens spectrometry. The peculiarities of analytical reactions at the nanogram level of reactants can be studied using this method. Under the conditions of the competing reaction of ligand protonation, the overall stability constant for iron(II) chelate with 1,10-phenanthroline was determined at a level of n x 10(-7) mol L(-1), logbeta3 = 21.3+/-0.1. The rates of formation and dissociation of iron(II) tris-(1,10-phenanthrolinate) at a level of n x 10(-8) mol L(-1) were found to be (2.05+/-0.05) x 10(-2) min(-1) and (3.0+/-0.1) x 10(-3) min(-1), respectively. The conditions for the determination of iron(II) with 1,10-phenanthroline by thermal lensing were reconsidered, and ascorbic acid was shown to be the best reducing agent, which provided minimum and reproducible sample pretreatment. Changes in the conditions at the nanogram level improved both the selectivity and sensitivity of determination. The optimum measurement conditions for thermal lensing were determined not only by the absorption of the analyte and reagents, but also by the background absorption of the solvent. The limits of detection and quantification of iron(II) at 488.0 nm (excitation beam power 140 mW) are 1 x 10(-9) and 6 x 10(-9) mol L(-1), respectively; the reproducibility RSD for the range n x 10(-8)-n x 10(-6) mol L(-1) is 2-5%.