| Attributes | Values |
|---|
| rdf:type
| |
| Description
| - 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. (en)
- 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. (cs)
|
| Title
| - 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 (cs)
- Vitamin E amides, a new class of vitamin E analogues with enhanced proapoptotic activity (en)
|
| 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 (cs)
- Vitamin E amides, a new class of vitamin E analogues with enhanced proapoptotic activity (en)
|
| skos:notation
| - RIV/68378050:_____/05:00001334!RIV06-AV0-68378050
|
| http://linked.open.../vavai/riv/strany
| |
| http://linked.open...avai/riv/aktivita
| |
| http://linked.open...avai/riv/aktivity
| |
| http://linked.open...iv/cisloPeriodika
| |
| http://linked.open...vai/riv/dodaniDat
| |
| http://linked.open...aciTvurceVysledku
| |
| http://linked.open.../riv/druhVysledku
| |
| http://linked.open...iv/duvernostUdaju
| |
| http://linked.open...titaPredkladatele
| |
| http://linked.open...dnocenehoVysledku
| |
| http://linked.open...ai/riv/idVysledku
| - RIV/68378050:_____/05:00001334
|
| http://linked.open...riv/jazykVysledku
| |
| http://linked.open.../riv/klicovaSlova
| - vitamin E amides; apoptosis; anticancer agents (en)
|
| http://linked.open.../riv/klicoveSlovo
| |
| http://linked.open...odStatuVydavatele
| - DE - Spolková republika Německo
|
| http://linked.open...ontrolniKodProRIV
| |
| http://linked.open...i/riv/nazevZdroje
| - International Journal of Cancer
|
| http://linked.open...in/vavai/riv/obor
| |
| http://linked.open...ichTvurcuVysledku
| |
| http://linked.open...cetTvurcuVysledku
| |
| http://linked.open...UplatneniVysledku
| |
| http://linked.open...v/svazekPeriodika
| |
| http://linked.open...iv/tvurceVysledku
| - Neužil, Jiří
- Mahdavian, E.
- Salvatore, B. A.
- Chapmann, J.
- EyTina, J.
- Tomic-Vatic, A.
|
| http://linked.open...n/vavai/riv/zamer
| |
| issn
| |
| number of pages
| |
![[RDF Data]](/fct/images/sw-rdf-blue.png)
![[cxml]](/fct/images/cxml_doc.png)
![[csv]](/fct/images/csv_doc.png)
![[text]](/fct/images/ntriples_doc.png)
![[turtle]](/fct/images/n3turtle_doc.png)
![[ld+json]](/fct/images/jsonld_doc.png)
![[rdf+json]](/fct/images/json_doc.png)
![[rdf+xml]](/fct/images/xml_doc.png)
![[atom+xml]](/fct/images/atom_doc.png)
![[html]](/fct/images/html_doc.png)