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Synthesis and QSAR of novel heteroaromatic amides as potentially antitumor active compounds (CROSBI ID 590373)

Prilog sa skupa u zborniku | sažetak izlaganja sa skupa

Viskić, Marko ; Sović, Irena ; Bertoša, Branimir ; Ester, Katja ; Kralj, Marijeta ; Hranjec, Marijana ; Karminski-Zamola, Grace Synthesis and QSAR of novel heteroaromatic amides as potentially antitumor active compounds // 6th Summer School Medicinal Chemistry. Regensburg, 2012. str. 255-255

Podaci o odgovornosti

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

engleski

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

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].

amides ; quinolones ; antiproliferative activity ; QSAR

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Podaci o prilogu

255-255.

2012.

objavljeno

Podaci o matičnoj publikaciji

6th Summer School Medicinal Chemistry

Regensburg:

Podaci o skupu

6th Summer School Medicinal Chemistry

poster

26.09.2012-28.09.2012

Regensburg, Njemačka

Povezanost rada

Kemija