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Statements

Subject Item
n2:RIV%2F68378050%3A_____%2F05%3A00001334%21RIV06-AV0-68378050
rdf:type
skos:Concept n13:Vysledek
dcterms:description
Analogy vitamínu E, např. alfa-TOS, jsou proapoptotické látky se selektivní protinádorovou aktivitou. Molekula alfa-TOS obsahuje několik strukturně a funkčně odlišných skupin, které lze modifikovat k získání analogů s vyšší aktivitou. K získání analogů s vyšší apoptogenní účinností jsme připravili nové sloučeniny s esterovou vazbou nahrazenou amidovou vazbou. Všechny tyto analogy působily mnohem proapoptogenněji než jejich esterové protějšky a nejúčinnější byl alfa-tokoferylmaleylamid. Metylace volné karboxylové skupiny zcela zrušila apoptogenní aktivitu těchto sloučenin. Podobně jako esterové analogy vyvolávaly amidy apoptózu destabilizací mitochondrií. Vyšší účinnost amidů oproti esterům může být způsobena jejich vyšším podílem v lipidové fázi. Modifikace esterové vazby v látkách jako alfa-TOS tedy může být využita jako základ pro tvorbu nových analogů s vyšší účinností při likvidaci maligních buněk. Vitamin E analogues, e.g. alpha-TOS, are proapoptotic agents with selective antineoplastic activity. The alpha-TOS molecule comprises several structurally and functionally distinct moieties that can be modified to yield analogues with higher activity. To find analogues with higher apoptogenic efficacy, we prepared novel compounds with ester bond replaced by an amide bond. All these analogues were significantly more proapoptotic than their ester counterparts, the most effective being alpha-tocopheryl maleyl amide. Methylation of the free carboxylic group completely obliterated apoptogenic activity of the compounds. Similarly as ester analogues, the amides induced apoptosis by mitochondrial destabilization. Superiority of amides over the esters may be due to their higher partitioning into the lipid phase. Thus, modification of the ester bond of agents such as alpha-TOS can be used as a basis for generating novel analogues with higher efficacy of killing malignant cells. Vitamin E analogues, e.g. alpha-TOS, are proapoptotic agents with selective antineoplastic activity. The alpha-TOS molecule comprises several structurally and functionally distinct moieties that can be modified to yield analogues with higher activity. To find analogues with higher apoptogenic efficacy, we prepared novel compounds with ester bond replaced by an amide bond. All these analogues were significantly more proapoptotic than their ester counterparts, the most effective being alpha-tocopheryl maleyl amide. Methylation of the free carboxylic group completely obliterated apoptogenic activity of the compounds. Similarly as ester analogues, the amides induced apoptosis by mitochondrial destabilization. Superiority of amides over the esters may be due to their higher partitioning into the lipid phase. Thus, modification of the ester bond of agents such as alpha-TOS can be used as a basis for generating novel analogues with higher efficacy of killing malignant cells.
dcterms:title
Vitamin E amides, a new class of vitamin E analogues with enhanced proapoptotic activity Vitamin E amides, a new class of vitamin E analogues with enhanced proapoptotic activity Amidy vitamínu E, nová třída analogů vitamínu E se zesílenou proapoptotickou aktivitou
skos:prefLabel
Vitamin E amides, a new class of vitamin E analogues with enhanced proapoptotic activity Amidy vitamínu E, nová třída analogů vitamínu E se zesílenou proapoptotickou aktivitou Vitamin E amides, a new class of vitamin E analogues with enhanced proapoptotic activity
skos:notation
RIV/68378050:_____/05:00001334!RIV06-AV0-68378050
n3:strany
118;193
n3:aktivita
n6:Z
n3:aktivity
Z(AV0Z5052915)
n3:cisloPeriodika
2
n3:dodaniDat
n12:2006
n3:domaciTvurceVysledku
n16:4589874
n3:druhVysledku
n14:J
n3:duvernostUdaju
n5:S
n3:entitaPredkladatele
n15:predkladatel
n3:idSjednocenehoVysledku
548950
n3:idVysledku
RIV/68378050:_____/05:00001334
n3:jazykVysledku
n11:eng
n3:klicovaSlova
vitamin E amides; apoptosis; anticancer agents
n3:klicoveSlovo
n4:anticancer%20agents n4:vitamin%20E%20amides n4:apoptosis
n3:kodStatuVydavatele
DE - Spolková republika Německo
n3:kontrolniKodProRIV
[42D9E9022377]
n3:nazevZdroje
International Journal of Cancer
n3:obor
n17:EB
n3:pocetDomacichTvurcuVysledku
1
n3:pocetTvurcuVysledku
6
n3:rokUplatneniVysledku
n12:2005
n3:svazekPeriodika
117
n3:tvurceVysledku
Salvatore, B. A. Chapmann, J. Mahdavian, E. Tomic-Vatic, A. EyTina, J. Neužil, Jiří
n3:zamer
n8:AV0Z5052915
s:issn
0020-7136
s:numberOfPages
6