Naslov
DNA and RNA binding studies of novel amidine- and amidoxime-substituted heterocycles

Autori
Shanmugam, Suresh ; Radić Stojković, Marijana ; Maračić, Silvija ; Raić-Malić, Silvana

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

Izvornik
27th Croatian Meeting of Chemists and Chemical Engineers and 5th Symposium Vladimir Prelog: Book of Abstracts / Marković, Dean ; Meštrović, Ernest ; Namjesnik, Danijel ; Tomašić, Vesna - Zagreb : Hrvatsko kemijsko društvo, 2021, 178-178

Skup
27. hrvatski skup kemičara i kemijskih inženjera (27HSKIKI) ; 5. simpozij Vladimir Prelog

Mjesto i datum
Veli Lošinj, Hrvatska, 05.10.2021. - 08.10.2021

Vrsta sudjelovanja
Poster

Vrsta recenzije
Domaća recenzija

Ključne riječi
DNA and RNA binding ; amidine-substituted heterocycles ; amidoxime-substituted heterocycles ; UV/Vis ; fluorescence ; circular dichroism

Sažetak
DNA is a major target for a large number of anticancer drugs due to their crucial functions in cells. Based upon the antiproliferative activity, several compounds (Figure 1) from a series of novel amidine- and amidoxime-substituted heterocycles (Department of Organic Chemistry, Faculty of Chemical Engineering and Technology) were selected for the study with calf thymus DNA (ctDNA), alternating AT-DNA and AU-RNA. Assessing the binding strength and mode of binding of small molecule-DNA interactions was performed using UV / Vis, fluorescence and circular dichroism (CD) spectroscopy. All studied compounds showed a greater stabilization effect of AT-DNA compared to ctDNA and AU-RNA. Only a derivative possessing two imidazole moieties at the end of the heteroaromatic structure stabilizes both DNA and RNA. The addition of some compounds to DNA solutions caused, either an appearance of positive induced CD spectra (ICD) or small negative ICD signals. Such changes in CD spectra suggest binding inside the DNA groove (positive ICD) or intercalative binding where the ligand is oriented ''parallel'' to the long axis of adjacent base pairs (negative ICD).

Izvorni jezik
Engleski

Znanstvena područja
Kemija

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