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https://open.uns.ac.rs/handle/123456789/19207
Title: | Biological evaluation of selected 3,4-dihydro-2(1H)-quinoxalinones and 3,4-dihydro-1,4-benzoxazin-2-ones: Molecular docking study | Authors: | Petronijević Jelena Janković Nenad Stanojković Tatjana P. Joksimović Nenad Grozdanić Nađa Vraneš Milan Aleksandar Tot Bugarčić Zorica |
Issue Date: | 2018 | Journal: | Archiv der Pharmazie | Abstract: | © 2018 Deutsche Pharmazeutische Gesellschaft In order to investigate new potential therapeutically active agents, we investigated the biological properties of two small libraries of quinoxalinones and 1,4-benzoxazin-2-ones. The results obtained showed that compounds 5, 9–11 have good cytotoxic activity against HeLa cells where the lowest IC50value (10.46 ± 0.82 μM/mL) was measured for compound 10. Additionally, the most active compounds (5, 9–11) showed much better selectivity for MRC-5 cells (up to 17.4) compared to cisplatin. In vitro evaluation of the inhibition of the enzyme α-glucosidase showed that compounds 10 and 11 exert significant inhibition of the enzyme at 52.54 ± 0.09 and 40.09 ± 0.49 μM, respectively. Competitive experiments with ethidium bromide (EB) indicated that all tested compounds have affinity to displace EB from the EB-DNA complex through intercalation, suggesting good competition with EB (Ksv= (3.1 ± 0.2), (5.1 ± 0.1), (5.6 ± 0.2), and (6.3 ± 0.2) × 103M−1). A molecular docking study was also performed to better understand the binding modes and to conclude the structure–activity relationships of the synthesized compounds. | URI: | https://open.uns.ac.rs/handle/123456789/19207 | ISSN: | 0365-6233 | DOI: | 10.1002/ardp.201700308 (BISIS)109428 |
Appears in Collections: | PMF Publikacije/Publications |
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