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Pregled bibliografske jedinice broj: 650840

The Novel [4, 5-e][1, 3]Diazepine-4, 8-dione and Acyclic Carbamoyl Imino-Ureido Derivatives of Imidazole : Synthesis, Anti-Viral and Anti-Tumor Activity Evaluations


Wittine, Karlo; Poljak, Kristina; Kovač, Matea; Makuc, Damjan; Plavec, Janez; Balzarini, Jan; Martinović, Tamara; Kraljević Pavelić, Sandra; Pavelić, Krešimir; Mintas, Mladen
The Novel [4, 5-e][1, 3]Diazepine-4, 8-dione and Acyclic Carbamoyl Imino-Ureido Derivatives of Imidazole : Synthesis, Anti-Viral and Anti-Tumor Activity Evaluations // Molecules, 18 (2013), 11; 13385-13397 doi:10.3390/molecules181113385 (međunarodna recenzija, članak, znanstveni)


Naslov
The Novel [4, 5-e][1, 3]Diazepine-4, 8-dione and Acyclic Carbamoyl Imino-Ureido Derivatives of Imidazole : Synthesis, Anti-Viral and Anti-Tumor Activity Evaluations

Autori
Wittine, Karlo ; Poljak, Kristina ; Kovač, Matea ; Makuc, Damjan ; Plavec, Janez ; Balzarini, Jan ; Martinović, Tamara ; Kraljević Pavelić, Sandra ; Pavelić, Krešimir ; Mintas, Mladen

Izvornik
Molecules (1420-3049) 18 (2013), 11; 13385-13397

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

Ključne riječi
Imidazole; [4; 5-e][1; 3]diazepine; anti-RSV; anti-tumor

Sažetak
In the present paper, we report on the synthesis, and in vitro antiviral and cytostatic activities of a series of novel imidazole[4, 5-e][1, 3]diazepine-4, 8-dione (compounds 9–11) and acyclic carbamoyl imino-ureido imidazole (compounds 12 and 13) derivatives. These new type of chemical entities showed no significant activity on the broad spectrum of DNA and RNA viruses. Results of antiproliferative assays performed on a panel of selected human tumor cell lines revealed that only compounds 1 and 5 showed moderate and selective cytostatic effect against HeLa cells (IC50 = 24 and 32 µM) with no concomitant cytotoxic effects on human normal fibroblasts (BJ). Importantly, an imidazole derivative containing a pyrrolidine moiety linked via an ethylenic spacer (3) showed a selective cytostatic effect toward cervical carcinoma (HeLa) cells (IC50 = 9.5 µM) with no apparent cytotoxicity on human normal fibroblasts (BJ). This compound can be therefore considered as a potential anti-tumor lead compound for further synthetic structure optimization.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Biotehnologija



POVEZANOST RADA


Projekt / tema
125-0982464-2922 - RAZVOJ NOVIH PROLIJEKOVA I LIJEKOVA PROTIV VIRUSA I RAKA (Mladen Mintas, )
335-0000000-3532 - Uloga IGF2 i signalni putovi nizvodno u karcinomima pluća čovjeka (Sandra Kraljević Pavelić, )
335-0982464-2393 - Molekularna obilježja miofibroblasta Dupuytrenove bolesti (Krešimir Pavelić, )

Ustanove
Fakultet kemijskog inženjerstva i tehnologije, Zagreb,
Sveučilište u Rijeci - Odjel za biotehnologiju

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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