Pregled bibliografske jedinice broj: 379982
Effect of 3, 4-Ethylenedioxy- Extension of Thiophene Core on the DNA/RNA Binding Properties and Biological Activity of Bis-Benzimidazole Amidines
Effect of 3, 4-Ethylenedioxy- Extension of Thiophene Core on the DNA/RNA Binding Properties and Biological Activity of Bis-Benzimidazole Amidines // Bioorganic & medicinal chemistry letters, 17 (2009), 6; 2544-2554 doi:10.1016/j.bmc.2009.01.071 (međunarodna recenzija, članak, znanstveni)
CROSBI ID: 379982 Za ispravke kontaktirajte CROSBI podršku putem web obrasca
Naslov
Effect of 3, 4-Ethylenedioxy- Extension of Thiophene Core on the DNA/RNA Binding Properties and Biological Activity of Bis-Benzimidazole Amidines
Autori
Stolić, Ivana ; Mišković, Katarina ; Magdaleno, Anahi ; Silber, Ariel Mariano ; Piantanida, Ivo ; Bajić, Miroslav ; Glavaš-Obrovac, Ljubica
Izvornik
Bioorganic & medicinal chemistry letters (0960-894X) 17
(2009), 6;
2544-2554
Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni
Ključne riječi
benzimidazole amidine ; DNA/RNA binding ; antiproliferative activity ; antiparasitic activity
Sažetak
Novel bisbenzimidazoles (4– 6), characterized by 3, 4-ethylenedioxy- extension of thiophene core, revealed pronounced affinity and strong thermal stabilization effect toward ds-DNA. They interact within ds-DNA grooves as dimmers or even oligomers and agglomerate along ds-RNA. Compounds 4– 6 have shown moderate to strong antiproliferative effect toward panel of eight carcinoma cell lines. Compound 5 displayed the best inhibitory potential and in equitoxic concentration (IC50 = 1 x 10– 6 M) induced accumulation of cells in G2/M phase after 48 h of incubation. Fluorescence microscopy showed that 5 entered into live HeLa cells within 30 min, but did not accumulate in nuclei even after 2.5 h. Compound 5 inhibited the growth of T. cruzi epimastigotes (IC50 = 4.3 x 10– 6 M).
Izvorni jezik
Engleski
Znanstvena područja
Kemija, Biologija, Temeljne medicinske znanosti
POVEZANOST RADA
Projekti:
053-0982914-2965 - Dizajn i sinteza bisamidina sa protutumorskim djelovanjem (Bajić, Miroslav, MZOS ) ( CroRIS)
098-0982914-2918 - Dizajn, sinteza i ispitivanje interakcija malih molekula s DNA, RNA i proteinima (Piantanida, Ivo, MZOS ) ( CroRIS)
219-0982914-2176 - Mehanizam bioloških učinaka novih malih molekula na stanice tumora čovjeka (Glavaš Obrovac, Ljubica, MZOS ) ( CroRIS)
219-0982914-2179 - Uloga malih zaštitinih TFF proteina u zdravlju i bolesti (Belovari, Tatjana, MZOS ) ( CroRIS)
Ustanove:
Veterinarski fakultet, Zagreb,
Institut "Ruđer Bošković", Zagreb,
Medicinski fakultet, Osijek
Profili:
Ivo Piantanida
(autor)
Miroslav Bajić
(autor)
Katarina Mišković Špoljarić
(autor)
Ljubica Glavaš Obrovac
(autor)
Ivana Stolić
(autor)
Citiraj 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
- MEDLINE