Synthesis, interaction with DNA and RNA and antitumor activity of diamidine derivatives of 3, 4-ethylenedioxythiophene-2, 5-dicarboxanilide (CROSBI ID 587874)
Prilog sa skupa u zborniku | sažetak izlaganja sa skupa | međunarodna recenzija
Podaci o odgovornosti
Stolić, Ivana ; Avdičević, Monika ; Piantanida, Ivo ; Glavaš-Obrovac, Ljubica ; Bajić, Miroslav
engleski
Synthesis, interaction with DNA and RNA and antitumor activity of diamidine derivatives of 3, 4-ethylenedioxythiophene-2, 5-dicarboxanilide
Related to our previous studies [1, 2] we have synthesized a series of novel diamidine derivatives of EDOT in order to examine influence of structure on interactions with polynucleotides (DNA/RNA) and their antiproliferative effects on on normal cells (MDCKI) and seven human tumour cell lines of different histological origin (HT-29, AGS, MIAPaCa2, CaCo2, HEp2, HeLa and NCI H358). Bisamide-amidine derivatives were prepared by amide bond formation between 3, 4-ethylenedioxythiophene-2, 5-dicarbonyl chloride and 3- or 4-aminobenzamidines. Interactions of novel compounds with ct-DNA and ds-RNA (poly A-poly U) were studied by UV/vis, CD and fluorescence spectrophotometry, as well as thermal melting experiments. Studies showed that affinity and binding mode of compound depend on the type and position of amidine moiety as well as on the ratio between concentration of compounds and polynucleotides. Generally, binding affinity of compounds 1-8 is higher toward ct-DNA compared to ds-RNA. At excess of compound over polynucleotide nonspecific aggolmeration interactions were observed. Antiproliferative effects depend on the applied concentration of the studied compound and type of treated cells.
amide-amidines ; 3 ; 4-ethylenedioxythiophene ; DNA/RNA binding ; antitumor activity
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Podaci o prilogu
P253-53.
2012.
objavljeno
Podaci o matičnoj publikaciji
Abstract CD: 13th Tetrahedron Symposium: Challenges in Bioorganic & Organic Medicinal Chemistry
L. Liu
Amsterdam:
Podaci o skupu
13th Tetrahedron Symposium: Challenges in Bioorganic & Organic Medicinal Chemistry
poster
26.06.2012-29.06.2012
Amsterdam, Nizozemska