Novel caffeine derivatives with antiproliferative activity

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F16%3A43875580" target="_blank" >RIV/60162694:G44__/16:43875580 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/00216208:11150/16:10323426 RIV/00179906:_____/16:10323426

Výsledek na webu

<a href="http://pubs.rsc.org/en/Content/ArticleLanding/2016/RA/C5RA22889A#!divAbstract" target="_blank" >http://pubs.rsc.org/en/Content/ArticleLanding/2016/RA/C5RA22889A#!divAbstract</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1039/c5ra22889a" target="_blank" >10.1039/c5ra22889a</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Novel caffeine derivatives with antiproliferative activity

Popis výsledku v původním jazyce

Caffeine is probably the best known and most widely used psychoactive substance in the world. Beside its psychoactive effects, caffeine has been found to affect the cell cycle and DNA repair, as a consequence of the inhibition of ATM and ATR kinases. These two DNA damage response kinases, members of the phosphatidylinositol 3-kinase related protein kinase family, represent very attractive anticancer drug targets. Their inhibition can selectively sensitize cancer cells to DNA damaging agents and even kill various tumour cells in monotherapy. We developed a series of caffeine derivatives and evaluated their antiproliferative effects on 11 human tumour cell lines and compared them against caffeine and a standard ATR inhibitor VE-821. Although the new caffeine derivatives did not achieve the overall potency of VE-821, several compounds exhibited enhanced antiproliferative activity compared to caffeine and in some cell lines showed at least comparable activity to VE-821.

Název v anglickém jazyce

Novel caffeine derivatives with antiproliferative activity

Popis výsledku anglicky

Caffeine is probably the best known and most widely used psychoactive substance in the world. Beside its psychoactive effects, caffeine has been found to affect the cell cycle and DNA repair, as a consequence of the inhibition of ATM and ATR kinases. These two DNA damage response kinases, members of the phosphatidylinositol 3-kinase related protein kinase family, represent very attractive anticancer drug targets. Their inhibition can selectively sensitize cancer cells to DNA damaging agents and even kill various tumour cells in monotherapy. We developed a series of caffeine derivatives and evaluated their antiproliferative effects on 11 human tumour cell lines and compared them against caffeine and a standard ATR inhibitor VE-821. Although the new caffeine derivatives did not achieve the overall potency of VE-821, several compounds exhibited enhanced antiproliferative activity compared to caffeine and in some cell lines showed at least comparable activity to VE-821.

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

—

Projekt

—

Návaznosti

S - Specificky vyzkum na vysokych skolach

Rok uplatnění

2016

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

RSC Advances

ISSN

2046-2069

e-ISSN

—

Svazek periodika

6

Číslo periodika v rámci svazku

39

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

6

Strana od-do

32534-32539

Kód UT WoS článku

000374045900016

EID výsledku v databázi Scopus

—