Anthraquinone-chalcone hybrids: Synthesis, preliminary antiproliferative evaluation and DNA-interaction studies
2015
Аутори:
Markovic, VioletaDebeljak, Nevena
Stanojkovic, Tatjana
Kolundzija, Branka
Sladic, Dusan
Vujcic, Miroslava
Janovic, Barbara
Tanić, Nikola
Perovic, Milka
Tesic, Vesna
Antic, Jadranka
Joksovic, Milan D.
Тип документа:
Чланак у часопису (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт:
Novel anthraquinone based chalcone compounds were synthesized starting
from 1-acetylanthraquinone in a Claisen-Schmidt reaction and evaluated
for their anticancer potential against three human cancer cell lines.
Compounds 4a, 4b and 4j showed promising activity in inhibition of HeLa
cells with IC50 values ranging from 2.36 to 2.73 mu M and low
cytotoxicity against healthy MRC-5 cell lines. The effects that
compounds produces on the cell cycle were investigated by flow
cytometry. It was found that 4a, 4b and 4j cause the accumulation of
cells in the S and G2/M phases in a dose-dependent manner and induce
caspase-dependent apoptosis. All of three compounds exhibit calf thymus
DNA-binding activity. The determined binding constants by absorption
titrations (2.65 x 10(3) M-1, 1.36 x 10(3) M(-1)and 2.51 x 10(3) M-1 of
4a/CT-DNA, 4b/CT-DNA and 4j/CT-DNA, respectively) together with
fluorescence displacement analysis designate 4a, 4b and 4j as strong
minor groove binders, but no cleavage of plasmid DNA was observed. (C)
2014 Elsevier Masson SAS. All rights reserved.
Кључне речи:
Chalcone; Anthraquinone; Cytotoxicity; ApoptosisИзвор:
European Journal of Medicinal Chemistry, 2015, 89, 401-410
DOI: 10.1016/j.ejmech.2014.10.055
ISSN: 1768-3254