Synthesis and QSAR of novel heteroaromatic amides as potentially antitumor active compounds (CROSBI ID 590373)
Prilog sa skupa u zborniku | sažetak izlaganja sa skupa
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