| Autor: |
Bondžić BP; Center for Chemistry, ICTM, University of Belgrade, P.O. Box 815, 11000 Belgrade, Serbia., Džambaski Z; Center for Chemistry, ICTM, University of Belgrade, P.O. Box 815, 11000 Belgrade, Serbia., Kolarević A; Department of Pharmacy, Faculty of Medicine, University of Niš, Bulevar Dr Zorana Đinđića 81, 18000 Niš, Serbia., Đorđević A; Department of Chemistry, Faculty of Science & Mathematics, University of Niš, Višegradska 33, 18000 Niš, Serbia., Anderluh M; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ljubljana, Aškerčeva cesta 7, 1000 Ljubljana, Slovenia., Šmelcerović A; Department of Pharmacy, Faculty of Medicine, University of Niš, Bulevar Dr Zorana Đinđića 81, 18000 Niš, Serbia. |
| Abstrakt: |
Aim: Eight new benzocyclobutane-2,5-diones ( 1a - 1h ) were synthesized, and their inhibitory properties against bovine pancreatic DNase I were examined in vitro . Methods & results: Compounds 1a - 1h were synthesized using photocycloaddition of duroquinone with various phenyl-substituted ethylenes in the presence of 18W compact fluorescent lamp (visible light). Two compounds, 1,3,4,6-tetramethyl-7-phenylbicyclo[4.2.0]oct-3-ene-2,5-dione ( 1a ) and 1,3,4,6-tetramethyl-7-p-tolylbicyclo[4.2.0]oct-3-ene-2,5-dione ( 1b ) inhibited DNase I in a noncompetitive manner with IC 50 values below 150 μM and showed to be more potent DNase I inhibitors than crystal violet, used as a positive control. In order to analyze potential binding sites for the studied compounds with DNase I, molecular docking study was performed. Conclusion: The studied benzocyclobutane-2,5-diones offer a good starting point for a design of new DNase I inhibitors. |
