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Novel symmetric bis-benzimidazoles: Synthesis, DNA/RNA binding and antitrypanosomal activity


Bistrović Popov, Andrea; Stolić, Ivana; Krstulović, Luka; Taylor, Martin; Kelly, John; Tomić, Sanja; Tumir, Lidija-Marija; Bajić, Miroslav; Raić-Malić, Silvana
Novel symmetric bis-benzimidazoles: Synthesis, DNA/RNA binding and antitrypanosomal activity // European journal of medicinal chemistry, 173 (2019), 63-75 doi:10.1016/j.ejmech.2019.04.007 (međunarodna recenzija, članak, znanstveni)


Naslov
Novel symmetric bis-benzimidazoles: Synthesis, DNA/RNA binding and antitrypanosomal activity

Autori
Bistrović Popov, Andrea ; Stolić, Ivana ; Krstulović, Luka ; Taylor, Martin ; Kelly, John ; Tomić, Sanja ; Tumir, Lidija-Marija ; Bajić, Miroslav ; Raić-Malić, Silvana

Izvornik
European journal of medicinal chemistry (0223-5234) 173 (2019); 63-75

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
Bis-benzimidazoles ; ctDNA binding ; UV-Vis ; CD spectroscopy ; thermal denaturation ; Trypanosoma brucei

Sažetak
The novel benzimidazol-2-yl-fur-5-yl-(1, 2, 3)- triazolyl dimeric series with aliphatic and aromatic central linkers was successfully prepared with the aim of assessing binding affinity to DNA/RNA and antitrypanosomal activity. UV-Visible spectroscopy, thermal denaturation showed interaction of heterocyclic bis-amidines with ctDNA. Circular dichroism studies indicated uniform orientation of heterocyclic bis-amidines along the chiral double helix axis, revealing minor groove binding as the dominant binding mode. The amidino fragment and 1, 4- bis(oxymethylene)phenyl spacer were the main determinants of activity against Trypanosoma brucei. The bis-benzimidazole imidazoline 15c, which had antitrypanosomal potency in the submicromolar range and DNA interacting properties, emerged as a candidate for further structural optimization to obtain more effective agents to combat trypanosome infections.

Izvorni jezik
Engleski

Znanstvena područja
Kemija



POVEZANOST RADA


Projekt / tema
HRZZ-IP-2018-01-4682 - Novi spojevi temeljeni na bioizosterima purina za ispitivanje njihovih antitumorskih i antipatogenih djelovanja (Silvana Raić-Malić, )

Ustanove
Veterinarski fakultet, Zagreb,
Institut "Ruđer Bošković", Zagreb,
Fakultet kemijskog inženjerstva i tehnologije, Zagreb

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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