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Novel thiosemicarbazone derivatives as potential antitumor agents: synthesis, physico-chemical and structural properties, DNA interactions and antiproliferative activity


Đilović, Ivica; Rubčić, Mirta; Vrdoljak, Višnja; Kraljević Pavelić, Sandra; Kralj, Marijeta; Piantanida, Ivo; Cindrić, Marina
Novel thiosemicarbazone derivatives as potential antitumor agents: synthesis, physico-chemical and structural properties, DNA interactions and antiproliferative activity // Bioorganic & Medicinal Chemistry, 16 (2008), 9; 5189-5198 doi::10.1016/j.bmc.2008.03.006 (međunarodna recenzija, članak, znanstveni)


Naslov
Novel thiosemicarbazone derivatives as potential antitumor agents: synthesis, physico-chemical and structural properties, DNA interactions and antiproliferative activity

Autori
Đilović, Ivica ; Rubčić, Mirta ; Vrdoljak, Višnja ; Kraljević Pavelić, Sandra ; Kralj, Marijeta ; Piantanida, Ivo ; Cindrić, Marina

Izvornik
Bioorganic & Medicinal Chemistry (0960-894X) 16 (2008), 9; 5189-5198

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

Ključne riječi
Thiosemicarbazone; antitumor evaluation; UV/vis spectroscopy; DNA binding

Sažetak
The paper describes synthesis of several novel thiosemicarbazone derivatives. Furthermore, crystal and molecular structure of 4-diethylamino-salicylaldehyde 4- phenylthiosemicarbazone revealed planarity of conjugated aromatic system, which suggested the possibility of DNA binding by intercalation, especially for here studied naphthalene derivatives. However, here presented DNA binding studies excluded this mode of action. Physicochemical and structural properties of novel derivatives were compared with previously studied analogues, taken as reference compounds, revealing distinctive differences. In addition, novel thiosemicarbazone derivatives (1, 2 and 5-8) clearly display stronger antiproliferative activity on five tumor cell lines than the reference compounds 3 and 4, which supports their further investigation as potential antitumor agents.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti



POVEZANOST RADA


Projekt / tema
098-0982464-2514 - Uloga različitih mehanizama odgovora stanica na terapiju oštećenjem DNA (Marijeta Kralj, )
098-0982914-2918 - Dizajn, sinteza i ispitivanje interakcija malih molekula s DNA, RNA i proteinima (Ivo Piantanida, )
119-1191342-1082 - Novi kompleksni spojevi i materijali-kemijski i biološki katalizatori (Marina Cindrić, )
119-1193079-1084 - Strukturno istraživanje bioloških makromolekula metodom rentgenske difrakcije (Dubravka Matković-Čalogović, )

Ustanove
Institut "Ruđer Bošković", Zagreb,
Prirodoslovno-matematički fakultet, 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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