- Synthesis and biological evaluation of novel aliphatic amido-quaternary ammonium salts for anticancer chemotherapy: Part i
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We synthesized novel aliphatic amido-quaternary ammonium salts in an effort to discover anticancer agents that increase Ras homolog gene family, member B, (RhoB) levels. These compounds exert anti-proliferative activities against several human cancer cell types. Seventeen compounds, varying in aliphatic carbon chain length and N-substituents, were synthesized and their biological activities were evaluated. Of these 17 compounds, compound 3i emerged as the most promising anticancer compound by promoting apoptosis through the RhoB mediated pathway. Potent biological activities observed for these novel aliphatic amido-quaternary ammonium salt analogues support their potential as anticancer, chemotherapeutic agents.
- Yang, Jee Sun,Song, Doona,Lee, Boah,Ko, Won Jin,Park, Song-Kyu,Won, Misun,Lee, Kiho,Kim, Hwan Mook,Han, Gyoonhee
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experimental part
p. 2861 - 2866
(2011/06/27)
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- Nematocidal activity of long alkyl chain amides, amines and their derivatives on dog roundworm larvae
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The nematocidal activity of amides and amines having a long alkyl chain against the second-stage larva of dog roundworm, Toxocara canis, was examined. Long chain acyl amides with smaller substituents on the nitrogen showed stronger activity and the activity of cyclic amine amides was stronger than that of acyclic ones. In a series of homologous amides, the activity was dependent on the alkyl chain length: it reached a maximum at an optimal chain length and decreased in both shorter and longer homologues. The relationship between the activity and hydrophobicity of the homologues was analysed by the use of the bilinear model. The hydrophobicity of a compound, which gives a maximal activity, was similar for all neutral amides, but amides which have an additional amine group in the molecule had different values. Tertiary amines and their salts having a long alkyl chain also showed nematocidal activities comparable to those of the corresponding amides. The salts killed the larva at concentrations lower than their critical micell concentration, suggesting that they behave as a single molecule for the nematocidal action.
- Kiuchi,Nishizawa,Kawanishi,Kinoshita,Ohsima,Uchitani,Sekino,Ishida,Kondo,Tsuda
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p. 3234 - 3244
(2007/10/02)
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- Transdermal compositions of 1-oxohydrocarbyl-substituted azacyclohexanes
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This invention provides compositions for enhancing penetration of physiologically active agents through the skin or mucosal membranes and for retaining these agents in body tissues, said composition comprising effective amounts of a physiologically-active agent and a compound represented by the general formula STR1 wherein X may represent sulfur, oxygen or nitrogen; a and b may be 0 or 1, c may be 0, 1 or 2, except that when X is oxygen, a, b and c are 0, when X is nitrogen c is 0 and only one of a or b is 1, and when X is sulfur a and b are 0; A is a branched or a straight chain, divalent aliphatic radical having from 0 to 2 double bonds; R' is selected from the group consisting of H, a lower alkyl group having from 1 to 4 carbon atoms, phenyl, lower alkyl or halogen substituted phenyl, acetamido, halogen, piperidinyl, lower alkyl or halogen substituted piperidinyl, carbalkoxy, carboxamide, and alkanoyl; and R is hydrogen or a lower alkyl group having from 1 to 4 carbon atoms, STR2 wherein R" is H or halogen, and salts, e.g. acid or quaternary derivatives, thereof. These compositions are useful in topical or transdermal applications of the physiologically-active agent.
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- Design of Neutral Hydrogen Ion Carriers for Solvent Polymeric Membrane Electrodes of Selected pH Range
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A series of new neutral carriers for hydrogen ions are used in solvent polymeric membrane (SPM) pH electrodes.Their dynamic pH range is directly related to the acidity constant of the active site of the ionophore.Further features for designing a SPM based pH electrode of broad and selected dynamic range are discussed.On this basis a neutral carrier based membrane electrode for hydrogen ions with a dynamic pH range from 8 to 0 is introduced.
- Oesch, Urs,Brzozka, Zbigniew,Xu, Aiping,Rusterholz, Bruno,Suter, Gabriela,et al.
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p. 2285 - 2289
(2007/10/02)
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