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Pregled bibliografske jedinice broj: 356728

Časopis

Autori: Hranjec, Marijana; Piantanida, Ivo; Kralj, Marijeta; Šuman, Lidija; Pavelić, Krešimir; Karminski-Zamola, Grace
Naslov: Novel amidino-substituted thienyl- and furyl-vinyl-benzimidazole derivatives and their photochemical conversion into corresponding diaza-cyclopenta[c]fluorenes. Synthesis, interactions with DNA and RNA and antitumor evaluation. Part 4.
Izvornik: Journal of Medicinal Chemistry (0022-2623) 51 (2008), 16; 4899-4910
Vrsta rada: članak
Ključne riječi: benzimidazoles; amidines; cyclopenta[c]fluorenes; interaction with DNA and RNA; antitumor evaluation
Sažetak:
Synthesis of novel non-fused amidino-substituted thienyl- and furyl-vinyl-benzimidazole derivatives and their photochemical cyclization into corresponding diaza-cyclopenta[c]fluorenes is described. All studied compounds showed prominent growth inhibitory effect. The fused compounds showed stronger activity than non-fused ones, whereby imidazolyl-substituted compound 11 proved to be the most active one. Besides, it induced strong G2/M arrest of the cell cycle followed by drastic apoptosis, which is in accordance with the DNA intercalative binding mode determined by the spectroscopic studies. Non-fused derivatives induced strong S phase arrest of the cell cycle followed by apoptosis that together with DNA minor groove binding mode, pointed to topoisomerase I inhibition. In addition, all non-fused compounds revealed pronounced selectivity toward tumor cells in comparison with non-tumor cells. Based on the presented results, both non-fused and fused tiophene-containing imidazolyl-derivatives should be considered as promising lead compounds for further investigation.
Projekt / tema: 098-0982914-2918, 098-0982464-2393, 098-0982464-2514, 125-0982464-1356
Izvorni jezik: ENG
Rad je indeksiran u
bazama podataka:
Current Contents Connect (CCC)
MEDLINE
Scopus
SCI-EXP, SSCI i/ili A&HCI
Science Citation Index Expanded (SCI-EXP) (sastavni dio Web of Science Core Collectiona)
Kategorija: Znanstveni
Znanstvena područja:
Kemija,Biologija,Temeljne medicinske znanosti
URL Internet adrese: http://pubs.acs.org/cgi-bin/abstract.cgi/jmcmar/asap/abs/jm8000423.html
URL cjelovitog teksta:
Google Scholar: Novel amidino-substituted thienyl- and furyl-vinyl-benzimidazole derivatives and their photochemical conversion into corresponding diaza-cyclopenta[c]fluorenes. Synthesis, interactions with DNA and RNA and antitumor evaluation. Part 4.
Upisao u CROSBI: mhranjec@fkit.hr (mhranjec@fkit.hr), 26. Svi. 2008. u 12:44 sati



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