Search

Three extracts were obtained from the aerial parts of meadowsweet ( Filipendula ulmaria (L.) Maxim.) using water, 40% ethanol, and 70% ethanol as extractants. Comparative assessment of their effect on the development of Lewis lung carcinoma (LLC) in C57Bl/6 line mice showed that, in isolated introduction, development of the metastatic process was inhibited by the extracts prepared in water and 70% ethanol, without influence on the growth of the tumor node. A comparative assessment of the effect of extracts on the antitumor effect of cyclophosphane (CPh) on the primary tumor node showed no changes in effectiveness of the cytostatic agent. When included in the treatment regimen of mice using extracts at a dose of 25 and 50 μg/kg, a significant increase in the antimetastatic action of CPh was detected under the influence of aqueous extract with metastasis inhibition index IMI = 75 and 98%, respectively, and with 70% ethanol extract (IMI = 95 and 96%). The effect of 40% ethanol extract on development of the tumor process in mice with LLC and the effectiveness of CPh therapy were not found.

Aim. Experimental evaluation of effect of E. coli LPS fractions on phagocyte and metabolic activity of blood neutrophils of laboratory mice with induced immune deficiency. Materials and methods. Phagocyte activity was evaluated by phagocyte number (PN), phagocyte index (PI) and integral phagocyte index (IPI), intensity of metabolism and energetic processes of enzyme systems - by test of tetrazolium nitro blue (TNB), mean cytochemical coefficient (MCC) in spontaneous and induced tests and stimulation index (SI). Results. LPS-3 substance administration into mice with secondary immune deficiency has resulted in a significantly highest increase of PN (15.8%), IPI (17.7%), TNB-IN (10.3%), cytochemical coefficients MCC-IN (u.) and IS (u.) - 14.8 and 10.9%, respectively, compared with the parameters of immune deficient mice that had received licopid. Conclusion. Some fractions of E. coli M17 polysaccharide have immune stimulating activity.

The efficacy of the combination treatment of P388 leukemia with cisplatin (cPt) and the platinum(IV) nitroxyl complex BC118 [e-ammine-d-(4-amino-2,2,6,6-tetramethylpiperidine-1-oxyl)-a,f-bis(acetato)-b,c-dichloroplatinum(iv)] applied in low doses was found to be synergistically increased. Thus, the use of 1/10 of their LD50 cured 100% of animals. The monotherapy with these drugs used in the same doses and at the same schedules showed moderate efficacy, and no animals survived. A synergistic increase in the toxicity was not observed. The rate of the development of resistance decreases in the series cPt+BC118, cPt, and BC118. Strains resistant to cPt+BC118 and BC118 are highly sensitive to doxorubicin, etoposide, and cyclophosphane.

The applicability of alkaline comet assay to studying the organ specificity of the genotoxic effects of drugs has been estimated using cells from four organs of mice (the liver, lungs, spleen, and brain). It has been found that cyclophosphamide damages DNA in all the four organs; and dioxidine, in all organs except the brain. It is concluded that this method can be used for studying the organ specificity of the DNA-damaging effects of various substances.

Es wird uber die Bildung von tBu2PP = P · (R)tBu2a und (tBu2P)2PR b, R = Me, Et, nPr, iPr, nBu, PhCH2, CH2CH = CH2, CF3 bei Umsetzungen von Li(THF)2 · [η2-(tBu2P)2P] 2 mit MeCl, MeI, EtCl, EtBr, nPrCl, nPrBr, iPrCl, nBuBr, PhCH2Cl, ClCH2CH = CH2 und CF3Br berichtet. Neben den ylidischen Verbindungen a bilden sich die entsprechenden Triphosphane (tBu2P)2PR b, wobei in THF-Losung die Bildung von a, in Pentan-Losung die von b begunstigt ist. Mit ClCH2CH2 = CH2 bildet sich nur b, mit CF3Br dagegen die Ylide tBu2PP = P(Br)tBu2 und tBu2PPP(CF3)tBu2, aber kein Phosphan b. Das Verhaltnis zwischen a und b wird auch durch die Reaktionstemperatur beeinflust. So bildet 2 mit EtBr in THF bei −70°C die Produkte tBu2PP = P(Et)tBu24a und (tBu2P)2PEt 4 b im Verhaltnis 4:3, bei 20°C 1:1; in Pentan bei −70°C 4a:4b = 1:1, bei 20°C 1:2. 2reagiert nicht mit tBuCl und H2C = CHCl. Die Verbindungen a zersetzen sich bei UV-Bestrahlung oder beim Erwarmen unter Bildung von tBu2PR und der Cyclophosphane (tBu2P)nPn. The Phosphinophosphinidene-phosphoranes tBu2PP = P(R)tBu2 from Li(THF)2[η2-(tBu2P)2P] and Alkyl Halides We report the formation of tBu2PP = P(R)tBu2a and (tBu2)2PR b (with R = Me, Et, nPr, iPr, nBu, PhCH2, H2C = CHCH2 and CF3) reactions of Li(THF)2[η2-(tBu2P)2P] 2 with MeCl, MeI, EtCl, EtBr, nPrCl, nPrBr, iPrCl, nBuBr, PhCH2Cl, H2C = CHCH2Cl or CF3Br. In THF solutions the ylidic compounds a predominate, whereas in pentane the corresponding triphosphanes b are preferrably formed. With ClCH2CH = CH2 only b is produced; CF3Br however yields both tBu2PP = P(Br)tBu2 and tBu2PP = P(CF3)tBu2, but no b. The ratio of a:b is influenced by the reaction temperature, too. The compounds tBu2PP = P(Et)tBu24a and (tBu2P)2PEt 4 b, e. g., are produced in a ratio of 4:3 at −70°C in THF, and 1:1 at 20°C; whereas 1:1 is obtained at −70°C in pentane, and 1:2 at 20°C. Neither tBuCl nor H2C = CHCl react with 2. The compounds a decompose thermally or under UV irradiation forming tBu2PR and the cyclophosphanes (tBu2P)nPn.

The effects of various energy metabolism modifiers and their combinations on cyclophosphane toxicity are examined in the fresh-water crustaceaDaphnia magna. The role of acute energy deficiency in the development of paralyzing effect of cyclophosphane is demonstrated. Transporting forms of succinic acid and combinations of carbonic acids with NAD exhibit high protective activity, while glucose reduces protective activity of NAD and sensitizing activity of amino acids.

Phenylcyclophosphane werden durch Tetrachlorkohlenstoff zum Chlor-trichlormethyl-phosphin 2a, Tetracyclohexylcyclotetraphosphan zum Diphosphan 3 abgebaut. Methyl-und Athylcyclophosphane bilden mit Tetrachlorkohlenstoff die monoquartaren Salze 4c bzw. 4d. Daneben entstehen die Spaltprodukte 5 bzw. 2d und 6. Durch die Einwirkung von Aminen auf Cyclophosphane und Tetrachlorkohlenstoff werden die Tris(amino)-phosphoniumsalze 7a,/–j und das Chlormethylphosphoniumchlorid 8a erhalten. Alle Phosphoniumchloride werden als Per-chlorate isoliert und charakterisiert. The Reaction of Cyclophosphanes with Carbon Tetrachloride and Amines The cleavage of phenylcyclophosphanes with carbon tetrachloride leads to the chloro-trichloromethyl-phosphine 2a; tetracyclohexycyclotetraphosphine decomposes in the same manner to the diphosphane 3. Methyl-and ethylcyclophosphanes give with carbon tetrachloride the monoquaternary salts 4c and 4d. The cleavage products 5, 2d and 6 are also formed. The tris-(amino)-phosphonium salts 7a–j and the chloromethylphosphonium chloride 8a are obtained by reaction of amines with cyclophosphanes and carbon tetrachloride. All phosphonium chlorides are isolated and charakterized as perchlorates.

Die Reaktionen von π-C5H5(CO)3MH (M = Cr, Mo, W) 1a–c mit den symmetrischen Diphosphanen (Ph2P)2, [Ph(CN)P]2 und [(CN)2P]2 laufen ebenso wie die mit dem Cyclophosphan (PPh)5 unter Spaltung der PP-Bindung ab. Die Reaktivitat nimmt in den Reihen ab. Die Tendenz zur Bildung zweikerniger Komplexe spiegelt die Basizitat der metallierten Phosphane π-C5H5(CO)3MPRR′ wider und steigt in der Folge P(CN)2 < P(CN)Ph ≪ P(Ph)H < PPh2 an. Iodhaltige Diphosphane [Ph(I)PP(I)Ph und P2I4] reagieren mit 1a–c unter Reduktion und Bildung von π-C5H5(CO)3MI und instabilen Iodo-diphosphanen. Keine PP-Bindungsspaltung tritt bei der Umsetzung der silylsubstituierten Diphosphane [Ph(Me3Si)P]2 und [(Me3Si)2P]2 mit 1a–c auf; bevorzugte Reaktion ist hier unter Bildung von π-C5H5(CO)3MSiMe3 die PSi-Bindungs-spaltung. Perfluoromethyl Element Ligands. XXXII. Reactions of the Metal Hydrides π-C5H5(CO)3MH (M = Cr, Mo, W) with Diphosphanes [Ph2−nYnP]2 (Y = I, CN, SiMe3; n = 2, 1, 0) The reactions of π-C5H5(CO)3MH (M = Cr, Mo, W) (1a–c) with the symmetric diphosphanes (Ph2P)2, [Ph(CN)P]2, [(CN)2P]2, and the cyclophosphane (PPh)5, respectively, occur under cleavage of the PP bond. The reactivity decreases in the series The tendency to form binuclear complexes reflects the basicity of the metallated phosphanes π-C5H5(CO)3MPRR′ and increases in the order P(CN)2 < P(CN)Ph ≪ P(Ph)H < PPh2. Iodine containing diphosphanes [Ph(I)PP(I)Ph and P2I4] undergo redox reactions with 1a–c, yielding π-C5H5(CO)3MI and unstable iodo-diphosphanes. No PP bond cleavage occurs in the reaction of the silyl substituted diphosphanes [Ph(SiMe3)P]2 and [(Me3Si)2P]2 with 1a–c, but PSi bond fission is the preferred reaction giving π-C5H5(CO)3MSiMe3.

Die Reaktion von K(tBu)P–P(tBu)K mit Isocyanid-dichloriden fuhrt zu den ersten Diphosphiraniminen (tBuP)2CNR. Daneben entstehen die Cyclophosphane (tBuP)n (n=3,4) und die entsprechenden zwei konfigurationsisomeren 1,3-Diphosphetan-2,4-diimine. N-Arylsubstituierte Diphosphiranimine mit einem voluminosen Substituenten in ortho-Position zur Iminofunktion, wie (tBuP)2CN(2,4-tBu2C6H3) (1) und (tBuP)2CN(2-tBuC6H4) (2), sind bei Raumtemperatur bestandig und konnten in reiner Form isoliert werden. Die Darstellung der Isocyanid-dichloride 2,4-tBu2C6H3NCCl2 und 2-tBuC6H4NCCl2 wird beschrieben. The reaction of K(tBu)P–P(tBu)K with isocyanide dichlorides yields the first diphosphiranimines (tBuP)2CNR. Besides, the cyclophosphanes (tBuP)n (n=3,4) and the two configurational isomers of the corresponding 1,3-diphosphetane-2,4-diimines are formed. N-Aryl-substituted diphosphiranimines with one bulky substituent in ortho-position to the imino function, such as (tBuP)2CN(2,4-tBu2C6H3) (1) and (tBuP)2CN(2-tBuC6H4) (2), are stable at room temperature and could be isolated in the pure state. The preparation of the isocyanide dichlorides 2,4-tBu2C6H3NCCl2 and 2-tBuC6H4NCCl2 is described.

Hexachlorcyclohexaphosphan (1) und Hexabromcyclohexaphosphan (2) werden bei der partiellen Enthalogenierung von Phosphor(III)-chlorid bzw. Phosphor(III)-bromid mit Magnesium oder Lithiumhydrid in polaren Solventien gebildet. Sie sind als erste perhalogenierte Cyclophosphane nur in verdunnter Losung bei tiefer Temperatur bestandig und konnten massenspektrometrisch und 31P-NMR-spektroskopisch charakterisiert werden. Wie das schon bekannte Hexaphenylcyclohexaphosphan, aber im Unterschied zur „Stammverbindung” P6H6, enthalten 1 und 2 ein Phosphor-Sechsringgerust, das offenbar durch elektronegative Substituenten stabilisiert wird. Contributions to the Chemistry of Phosphorus, 1881). – Halogen-Substituted Cyclohexaphosphanes: Formation and Properties of (PCl)6 and (PBr)6 Hexachlorocyclohexaphosphane (1) and hexabromocyclohexaphosphane (2) are formed in the partial dehalogenation of phosphorus trichloride and phosphorus tribromide, respectively, by magnesium or lithium hydride in polar solvents. As the first perhalogenated cyclophosphanes they are only stable in diluted solutions at low temperature and could be characterized by means of mass spectrometry and 31P nuclear magnetic resonance. Like the known hexaphenylcyclohexaphosphane, but in contrast to the „parent compound” P6H6, 1 and 2 have a six-membered phosphorus ring skeleton, which is obviously stabilized by electronegative substituents.