[Antimitotic activity of new 2,6-dinitroaniline derivatives and their synergistic activity in compositions with graminicides].

Shown antimicrotrubules activity of new 2,6-dinitroaniline compounds. Investigated their ability on apoptotic processes in a plant cell when used as a composition with inhibitors of acetyl-CoA carboxylase.

[Structural-biological characteristics of tubulin interaction with dinitroanilines].

The interaction of dinitroaniline compounds with tubulin molecules is characterized by extraordinary selectivity--these matters effectively associate with plant as well as protozoan tubulin and practically don't interact with fungal and animal tubulin in spite of extraordinarily high level of similarity of their sequences. Structural features and mechanisms of this interaction are generalized and in detail analysed in this research. In particular, the regularities of dinitroaniline binding sites' structure and localization on surfaces of tubulin different subunits and tubulins of different origin are characterized. Dinitroaniline binding sites are disposed on the surfaces of longitudinal contacts between tubulin subunits, contain residues of diamine amino acids (lysine or arginine) coupling al nitrile group (s) of dinitroanilines. Binding site location on the surfaces of the same subunit of different origin (for example, plant and protozoan alpha-tubulins) is coincided, however site localisation on surface of alpha- and beta-subunits is distinct. The described sites potentially can be the binding areas for another antimicrotubular compounds, in particular, cyanoacrilates.

[Screening of new 2,4- and 2,6-dinitroaniline derivates for phytotoxicity and antimitotic activity].

The results of Allium-test screening of new 2,4- and 2,6-dinitroaniline derivates on antimitotic activity and phytotoxicity are presented in the work. It is revealed that all studied compounds which are derivates of 2,4-dinitroaniline, 2,6-dinitro-(4-fluoromethyl)-aniline as well as (methylsulfonyl) nitrobenzol, can evoke a change in mitotic index value, an appearance of cytogenetic damages and also have phytotoxic effect on Allium cepa seedling roots. On data obtained the continuation of investigation the action of N-(2,4-dinitrophenyl)-orto-aminobenzoic acid, N,N-diethyl-2,6-dinitro-4-(trifluoromethyl)-aniline and 1-methylsulfonyl-3-nitrobenzol as potential herbicides is proposed.

[Inhibition of alkaline phosphatase by thioureido derivatives of methylenebisphosphonic acid].

A series of thioureido derivatives of methylenebisphosphonic acid were synthesized by the reaction of aminomethylenebisphosphonic acid with the corresponding isothiocyanates, and their effect on the activity of alkaline phosphatases from bovine small intestine mucosa (BSIM) and human placenta was studied. It was found that (3-phenylthioureido)methylenebisphosphonate is approximately one order of magnitude more effective in inhibiting the activity of alkaline phosphatase from BSIM than the alkyl derivatives of thioureidomethylenebisphosphonic acid with methyl, ethyl, tert-butyl, or cyclohexyl substituents. The introduction of substituents into the benzene ring of (3-phenylthioureido)methylenebisphosphonate decreased the effect of the inhibitor on the activity of the enzyme. The affinity of (3-phenylureido)methylenebisphosphonate to the alkaline phosphatase of BSIM was also weaker as compared with the corresponding thioureidomethylenebisphosphonate. The insertion of thioureidobisphosphonates into the active site of alkaline phosphatase of human placenta by the method of molecular docking indicated that the methylenebisphosphonate residue and the substituted amino groups of the inhibitor are involved in the mechanisms of complex formation with the enzyme. It is supposed that the improvement of the inhibitory activity of (3-phenylthioureido)methylenebisphosphonate toward alkaline phosphatase of BSIM is due to the additional fixation of the phenyl substituent in the active site of the enzyme.

[Combined effect of Pb2+ and divalent mental complexes on superprecipation and ATPase activity of myometrial actomyosin]. / Sochetanoe deistvie Pb2+ i kompleksonov dvukhvalentnykh metallov na superpretsipitatsiiu i ATP-aznuiu aktivnost aktomiozina miometriia.

The inhibiting effect of Pb2+ (0.1-1.0 mM) on superprecipitation and ATPase activity of myometrium actomyosin has been shown. It is found out that of 11 studied chelators of bivalent cations only monosodium salt of 4-guanidino-1-hydroxybutyliden-1.1-bisphosphonic acid can efficiently renews the value of superprecipitation and ATPase activity of actomyosin in presence of lead ions. It is supposed that this renewal is underlied by binding of guanidin group of Pb ions.

[Anti-androgenic activity of various substituted carboxyanilides]. / Antiandrogennaia aktivhost' nekotorykh zameshchennykh karboksianilidov.

The synthesis of 10 substituted carboxy anilides was performed and their antiandrogenic activity was investigated. It was shown, that 4-nitro-3-trifluoro-methyl-alpha-hydroxy-isobutyranilide, 4-nitro-3-trifluoro-methyl-isobutyranilide and 4-nitro-3-trifluoro-methyl-ethyl-methyl acetanilide exert the most pronounced antiandrogenic effects in experimental immature castrated male rats, given substituted doses of testosterone propionate. The antiandrogenic activity is mainly caused by the presence of trifluoro-methyl- and nitro-groups in meta- and para-positions of anilide benzene ring, as well as by hydroxyl group and hydrogen atom presence in alpha-carbon atom of the molecule alkyl moiety. A possible use of non-steroid antiandrogens for studying androgen mechanism of action and treating androgen-dependent diseases is discussed.

[Effect of ethylenediamine derivatives on Na+, K+-ATPase and K+-p-nitrophenyl phosphatase activity of brain enzyme preparations]. / O vliianii riada proizvodnykh etilendiamina na Na+, K+-ATP-aznuiu i K+-n-nitrofenilfosfataznuiu aktivnosti fermentnykh preparatov mozga.

The activity of Na+, K+-ATPase preparations was studied as affected by ethonium and its analogs. Ethonium is found to be able of producing a strong inhibitory effect on the Na+, K+-ATPase and K+-n-nitrophenyl phospnatase activities (I50 = 2.5.10(-5) and 6.5.10(-5) M, respectively). The inhibition is irreversible under experimental conditions and is reduced when the concentration of protein and sodium ions in the incubation medium rises. A dependence is found between the inhibitory effect of the analogs and the length of their hydrocarbon radical (the inhibition maximum corresponds to bisquarternary ammonium compound with the hydrocarbon radical consisting of 10 links) and some kinetic characteristics of this effect are studied. It is supposed that the mechanism of the inhibitory effect is due to the ethonim binding by the hydrocarbon radical in the preparation hydrophobic zone, the electrostatic interaction being not excluded.