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Pregled bibliografske jedinice broj: 642266

Biologically active heteroaromatic derivatives with amino side chains as potential anticancer agents


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
Biologically active heteroaromatic derivatives with amino side chains as potential anticancer agents // XXIIth National Meeting on Medicinal Chemistry : Abstract Book
Rim: Italian Chemical Society Division of Medicinal Chemistry, European Federation for Medicinal Chemistry, 2013. str. 77-78 (poster, međunarodna recenzija, sažetak, znanstveni)


Naslov
Biologically active heteroaromatic derivatives with amino side chains as potential anticancer agents

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

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
XXIIth National Meeting on Medicinal Chemistry : Abstract Book / - Rim : 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

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

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.

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, )
125-0982464-1356 - Novi heterocikli kao antitumorski i antivirusni ("pametni") lijekovi (Marijana Hranjec, )
335-0000000-3532 - Uloga IGF2 i signalni putovi nizvodno u karcinomima pluća čovjeka (Sandra Kraljević Pavelić, )

Ustanove
Institut "Ruđer Bošković", Zagreb,
Fakultet kemijskog inženjerstva i tehnologije, Zagreb,
Sveučilište u Rijeci - Odjel za biotehnologiju