Naslov
Synthesis and QSAR of novel heteroaromatic amides as potentially antitumor active compounds

Autori
Viskić, Marko ; Sović, Irena ; Bertoša, Branimir ; Ester, Katja ; Kralj, Marijeta ; Hranjec, Marijana ; Karminski-Zamola, Grace

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

Izvornik
6th Summer School Medicinal Chemistry / - Regensburg, 2012, 255-255

Skup
6th Summer School Medicinal Chemistry

Mjesto i datum
Regensburg, Njemačka, 26.09.2012. - 28.09.2012

Vrsta sudjelovanja
Poster

Vrsta recenzije
Nije recenziran

Ključne riječi
amides ; quinolones ; antiproliferative activity ; QSAR

Sažetak
The in vitro antiproliferative activities of 2- and 4-substituted quinolones is well known and these compounds represent a promising starting point in search for new anticancer agents [1-2]. A series of novel 2-benzimidazolyl-, 2-benzothiazolyl-, pyridyl- and phenylsubstituted amides was prepared. Photochemical procedures were used to prepare derivatives with fluorene and quinolone scaffolds which are cyclic analogues of prepared amides. In vitro antitumor activity tests performed against a panel of different cancer cell lines had shown activity of some compounds with notable examples being 1 (IC50/mM = 2.04), 2 (IC50/mM = 4.82) and 3 (IC50/mM = 1.51). Experimentally determined anticancer activities were used for building QSAR models for predicting antitumor activity of heterocyclic amides and quinolones. Similar approach for building QSAR models was already proven useful in understanding molecular properties with higher influence on antitumor activity in our previous studies [3].

Izvorni jezik
Engleski

Znanstvena područja
Kemija

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