Design and synthesis of novel 1,2,4-triazolo[4,3-b]pyridazine derivatives with anti-cancer activity

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F23%3A73619588" target="_blank" >RIV/61989592:15310/23:73619588 - isvavai.cz</a>

Výsledek na webu

<a href="https://www.sciencedirect.com/science/article/pii/S0022286023010323" target="_blank" >https://www.sciencedirect.com/science/article/pii/S0022286023010323</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.molstruc.2023.135938" target="_blank" >10.1016/j.molstruc.2023.135938</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Design and synthesis of novel 1,2,4-triazolo[4,3-b]pyridazine derivatives with anti-cancer activity

Popis výsledku v původním jazyce

Novel 1,2,4-triazolo[4,3-b]pyridazine derivatives (7a–d, 8a–m and 9a–i) were designed and synthesized in good to moderate yields. The synthesized compounds were characterized by spectroscopic studies (NMR and IR) and the fluorine coupled 13C NMR data for each synthesized series have also been explained. The compounds were evaluated for their in-vitro anti-proliferative activity against K562, MV4-11, G361 and HCC827 human cancer cell lines. Almost all the synthesised compounds were active against MV4-11 below 25 µM, especially 8l which showed activity with IC50 of 1.5 µM. Furthermore, compound 8l displayed anticancer activity against all four cancer cell lines tested with IC50 values ranging from 1.5 to 7.6 µM. In general, most of the compounds did not show any significant anti-proliferative activity against K562, G361 and HCC827 cells. Preliminary investigation of their effect on proliferation and viability of MV4-11 cells was carried out with 8l and the results indicate that the cells undergo a cell death with biochemical signs of apoptosis.

Název v anglickém jazyce

Design and synthesis of novel 1,2,4-triazolo[4,3-b]pyridazine derivatives with anti-cancer activity

Popis výsledku anglicky

Novel 1,2,4-triazolo[4,3-b]pyridazine derivatives (7a–d, 8a–m and 9a–i) were designed and synthesized in good to moderate yields. The synthesized compounds were characterized by spectroscopic studies (NMR and IR) and the fluorine coupled 13C NMR data for each synthesized series have also been explained. The compounds were evaluated for their in-vitro anti-proliferative activity against K562, MV4-11, G361 and HCC827 human cancer cell lines. Almost all the synthesised compounds were active against MV4-11 below 25 µM, especially 8l which showed activity with IC50 of 1.5 µM. Furthermore, compound 8l displayed anticancer activity against all four cancer cell lines tested with IC50 values ranging from 1.5 to 7.6 µM. In general, most of the compounds did not show any significant anti-proliferative activity against K562, G361 and HCC827 cells. Preliminary investigation of their effect on proliferation and viability of MV4-11 cells was carried out with 8l and the results indicate that the cells undergo a cell death with biochemical signs of apoptosis.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

10403 - Physical chemistry

Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

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

Rok uplatnění

2023

Kód důvěrnosti údajů

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

Název periodika

JOURNAL OF MOLECULAR STRUCTURE

ISSN

0022-2860

e-ISSN

1872-8014

Svazek periodika

1291

Číslo periodika v rámci svazku

NOV

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

10

Strana od-do

"135938-1"-"135938-10"

Kód UT WoS článku

001030635000001

EID výsledku v databázi Scopus

2-s2.0-85162870993