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Novel bis-phenanthridine derivatives with easily tunable linkers, study of their interactions with DNA and screening of antiproliferative activity


Dukši, Marko; Baretić, Domagoj; Čaplar, Vesna; Piantanida, Ivo
Novel bis-phenanthridine derivatives with easily tunable linkers, study of their interactions with DNA and screening of antiproliferative activity // European journal of medicinal chemistry, 45 (2010), 6; 2671-2676 doi::10.1016/j.ejmech.2010.02.017 (međunarodna recenzija, članak, znanstveni)


Naslov
Novel bis-phenanthridine derivatives with easily tunable linkers, study of their interactions with DNA and screening of antiproliferative activity

Autori
Dukši, Marko ; Baretić, Domagoj ; Čaplar, Vesna ; Piantanida, Ivo

Izvornik
European journal of medicinal chemistry (0223-5234) 45 (2010), 6; 2671-2676

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

Ključne riječi
Phenanthridine; solid phase synthesis; DNA binding; fluorescence

Sažetak
Series of novel peptide-bridged bis-phenanthridine derivatives as well as corresponding monomers were prepared by solid phase peptide synthesis, which allowed easy and fast tuning of compound properties. Interactions of new derivatives with double stranded DNA were strongly structure-dependent, among which the most interesting is bis-phenanthridine derivative forming intramolecular excimer, with specific fluorescence band sensitive to the pH as well as on the interactions with ds-DNA. Moreover, at variance to commonly high cytotoxic effects of phenanthridine derivatives, here studied monomeric as well as bis-phenanthridine derivatives exhibited negligible antiproliferative activity on a panel of human cell lines, which makes them promising lead compounds for development of new spectrophotometric markers.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti



POVEZANOST RADA


Projekt / tema
098-0982914-2918 - Dizajn, sinteza i ispitivanje interakcija malih molekula s DNA, RNA i proteinima (Ivo Piantanida, )

Ustanove
Institut "Ruđer Bošković", 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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