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Pregled bibliografske jedinice broj: 642266

Zbornik radova

Autori: Perin, Nataša; Aleksić, Maja; Sović, Irena; Hranjec, Marijana; Ester, Katja; Kralj, Marijeta; Ratkaj, Ivana; Kraljević Pavelić, Sandra; Nhili, Raja; David-Cordonnier, Marie-Hélène; Karminski-Zamola, Grace
Naslov: Biologically active heteroaromatic derivatives with amino side chains as potential anticancer agents
Izvornik: XXIIth National Meeting on Medicinal Chemistry : Abstract BookRim : Italian Chemical Society Division of Medicinal Chemistry, European Federation for Medicinal Chemistry , 2013. 77-78.
Skup: National Meeting on Medicinal Chemistry (13 ; 2013)
Mjesto i datum: Rim, Italija, 10.-13.09.2013.
Ključne riječi: benzimidazo[1; 2-a]quinolines; benzo[b]thieno[2; 3-c]quinolones; derivatives of isoindoline; antiproliferative activity; interaction with ct-DNA
Sažetak:
Over the past few years substituted heterocyclic derivatives have been one of the most extensively studied classes of organic compounds due to their well known biological activities. The development of effective antineoplastic drugs has become one of the most intensively studied aspects of contemporary medicinal chemistry and therefore has been tremendous growth in the number and types of new anticancer agents. One of the most used classes of chemotherapeutic agents in cancer therapy comprise molecules that interact with DNA, such as groove binders, DNA alkylating agents or intercalators. In this report we are presenting the synthesis and antitumor activity of some polyfunctional heterocyclic compounds regarding cyclic benzimidazole, quinolone and isoindoline derivatives bearing different amino side chains. For the synthesis of novel compounds were used classical methods of organic synthesis, photochemical cyclizations and microwave assisted reactions. Structures of prepared compounds were confirmed by means of 1H, 13C NMR, IR and UV spectroscopy. Antiproliferative activity in vitro was tested on several human tumor cell lines. Some of tested compounds showed a differential and significant antiproliferative effect at micromole concentrations. To shed more light on the mechanisms of biological action, additional experiments of interaction with ct-DNA of some active compounds were performed by using UV/Vis, fluorescence and CD spectroscopy and thermal melting experiments as well as topoisomerases I and II inhibition, cell cycle perturbances, subcellular localization and the influence on Enhanced Green Fluorescence protein.
Vrsta sudjelovanja: Poster
Vrsta prezentacije u zborniku: Sažetak
Vrsta recenzije: Međunarodna recenzija
Projekt / tema: 335-0000000-3532, 098-0982464-2514, 125-0982464-1356
Izvorni jezik: ENG
Kategorija: Znanstveni
Znanstvena područja:
Kemija,Temeljne medicinske znanosti
Upisao u CROSBI: Nataša Perin (nperin@fkit.hr), 17. Ruj. 2013. u 10:50 sati



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