A novel class of small molecule inhibitors with radioprotective properties

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00179906%3A_____%2F20%3A10409767" target="_blank" >RIV/00179906:_____/20:10409767 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/00216208:11150/20:10409767 RIV/60162694:G44__/20:00555635

Výsledek na webu

<a href="https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=Dn30pSHoZI" target="_blank" >https://verso.is.cuni.cz/pub/verso.fpl?fname=obd_publikace_handle&handle=Dn30pSHoZI</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.ejmech.2019.111606" target="_blank" >10.1016/j.ejmech.2019.111606</a>

Jazyk výsledku

angličtina

Název v původním jazyce

A novel class of small molecule inhibitors with radioprotective properties

Popis výsledku v původním jazyce

The goal of this study was to develop novel radioprotective agents targeting the intrinsic apoptotic pathway and thus decreasing the radiation-induced damage. For that purpose, we designed, synthesized and analyzed ten new compounds based on the 1-(4-(2-hydroxyethyl)piperazin-l-yl)-3-phenoxypropan-2-ol leading structure. The cytotoxicity of the newly synthesized substances was tested in vitro on cell lines derived from different progenitor cells by WST-1 proliferation assay. mTr test was utilized to assess half-maximal inhibitory concentrations and maximum tolerated concentrations of novel compounds in A-549 cells. Screening for radioprotective properties was performed using flow-cytometry in MOLT-4 cells exposed to Co-60 ionizing gamma radiation. Selected candidates underwent in vivo testing in C57BI/6J mice having a positive impact on their immunological status. In summary, we report here promising compounds with radioprotective effect in vivo. (C) 2019 Elsevier Masson SAS. All rights reserved.

Název v anglickém jazyce

A novel class of small molecule inhibitors with radioprotective properties

Popis výsledku anglicky

The goal of this study was to develop novel radioprotective agents targeting the intrinsic apoptotic pathway and thus decreasing the radiation-induced damage. For that purpose, we designed, synthesized and analyzed ten new compounds based on the 1-(4-(2-hydroxyethyl)piperazin-l-yl)-3-phenoxypropan-2-ol leading structure. The cytotoxicity of the newly synthesized substances was tested in vitro on cell lines derived from different progenitor cells by WST-1 proliferation assay. mTr test was utilized to assess half-maximal inhibitory concentrations and maximum tolerated concentrations of novel compounds in A-549 cells. Screening for radioprotective properties was performed using flow-cytometry in MOLT-4 cells exposed to Co-60 ionizing gamma radiation. Selected candidates underwent in vivo testing in C57BI/6J mice having a positive impact on their immunological status. In summary, we report here promising compounds with radioprotective effect in vivo. (C) 2019 Elsevier Masson SAS. All rights reserved.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

30104 - Pharmacology and pharmacy

Projekt

<a href="/cs/project/GA17-13541S" target="_blank" >GA17-13541S: Vývoj nových radioprotektivních látek na bázi malých molekulárních inhibitorů</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2020

Kód důvěrnosti údajů

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

Název periodika

European Journal of Medicinal Chemistry

ISSN

0223-5234

e-ISSN

—

Svazek periodika

187

Číslo periodika v rámci svazku

FEB

Stát vydavatele periodika

FR - Francouzská republika

Počet stran výsledku

11

Strana od-do

111606

Kód UT WoS článku

000510525000055

EID výsledku v databázi Scopus

2-s2.0-85077754376