Pregled bibliografske jedinice broj: 945992
Selenazolyl-hydrazones as Novel Selective MAO Inhibitors With Antiproliferative and Antioxidant Activities: Experimental and In-silico Studies
Selenazolyl-hydrazones as Novel Selective MAO Inhibitors With Antiproliferative and Antioxidant Activities: Experimental and In-silico Studies // Frontiers in Chemistry, 6 (2018), 247, 18 doi:10.3389/fchem.2018.00247 (međunarodna recenzija, članak, znanstveni)
CROSBI ID: 945992 Za ispravke kontaktirajte CROSBI podršku putem web obrasca
Naslov
Selenazolyl-hydrazones as Novel Selective MAO Inhibitors With Antiproliferative and Antioxidant Activities: Experimental and In-silico Studies
Autori
Elshaflu, Hana ; Todorović, Tamara R. ; Nikolić, Milan ; Lolić, Aleksandar ; Višnjevac, Aleksandar ; Hagenow, Stefanie ; Padrón, José M. ; García-Sosa, Alfonso T. ; Djordjević, Ivana S. ; Grubišić, Sonja ; Stark, Holger ; Filipović, Nenad R.
Izvornik
Frontiers in Chemistry (2296-2646) 6
(2018);
247, 18
Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni
Ključne riječi
selenazoles, MAO B, Anticancer activity, Docking, Antioxidant agents
Sažetak
The novel approach in the treatment of complex multifactorial diseases, such as neurodegenerative disorders and cancer, requires a development of efficient multi-targeting oriented drugs. Since oxidative stress significantly contributes to the pathogenesis of cancer and neurodegenerative disorders, potential drug candidates should possess good anti-oxidant properties. Due to promising biological activities shown for structurally related (1, 3-thiazol-2-yl)hydrazones, a focused library of twelve structurally related benzylidene-based (1, 3-selenazol-2-yl)hydrazones was designed as potential multi-targeting compounds. Monoamine oxidases (MAO) A/B inhibition properties of this class of compounds have been investigated. Surprisingly, the p-nitrophenyl-substituted (1, 3-selenazol-2-yl)hydrazone 4 showed MAO B inhibition in a nanomolar concentration range (IC50 = 73 nM). Excellent anti-oxidant properties were confirmed in a number of different in vitro assays. Antiproliferative activity screening on a panel of six human solid tumor cell lines showed that potencies of some of the investigated compounds was comparable or even better than that of the positive control 5-fluorouracil. In-silico calculations of ADME properties pointed to promising good pharmacokinetic profiles of investigated compounds. Docking studies suggest that some compounds, compared to positive controls, have the ability to strongly interact with targets relevant to cancer such as 5'-nucleotidase, and to neurodegenerative diseases such as the small conductance calcium-activated potassium channel protein 1, in addition to confirmation of inhibitory binding at MAO B.
Izvorni jezik
Engleski
Znanstvena područja
Kemija, Interdisciplinarne prirodne znanosti
POVEZANOST RADA
Ustanove:
Institut "Ruđer Bošković", Zagreb
Poveznice na cjeloviti tekst rada:
Pristup cjelovitom tekstu rada doi www.frontiersin.org fulir.irb.hrCitiraj ovu publikaciju:
Časopis indeksira:
- Current Contents Connect (CCC)
- Web of Science Core Collection (WoSCC)
- Science Citation Index Expanded (SCI-EXP)
- SCI-EXP, SSCI i/ili A&HCI
- Scopus
