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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


Stolić, Ivana; Mišković, Katarina; Magdaleno, Anahi; Silber, Ariel Mariano; Piantanida, Ivo; Bajić, Miroslav; Glavaš-Obrovac, Ljubica
Effect of 3, 4-Ethylenedioxy- Extension of Thiophene Core on the DNA/RNA Binding Properties and Biological Activity of Bis-Benzimidazole Amidines // Bioorganic and Medicinal Chemistry, 17 (2009), 6; 2544-2554 doi:10.1016/j.bmc.2009.01.071 (međunarodna recenzija, članak, znanstveni)


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 and Medicinal Chemistry (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


Projekt / tema
053-0982914-2965 - Dizajn i sinteza bisamidina sa protutumorskim djelovanjem (Miroslav Bajić, )
098-0982914-2918 - Dizajn, sinteza i ispitivanje interakcija malih molekula s DNA, RNA i proteinima (Ivo Piantanida, )
219-0982914-2176 - Mehanizam bioloških učinaka novih malih molekula na stanice tumora čovjeka (Ljubica Glavaš Obrovac, )
219-0982914-2179 - Uloga malih zaštitinih TFF proteina u zdravlju i bolesti (Tatjana Belovari, )

Ustanove
Veterinarski fakultet, Zagreb,
Institut "Ruđer Bošković", Zagreb,
Medicinski fakultet, Osijek

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


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