Opcije pristupačnosti Pristupačnost
Exploring the antioxidative potential of benzazole scaffold in the design of novel antitumor agents

Summary

The proposed scientific project is oriented towards the design and development of novel and efficient benzazole derivatives as antioxidants with antitumor activity as a part of antitumor therapeutic strategy based on inhibition of ROS. The project is highly multidisciplinary and brings together an interdisciplinary team of researchers whose common synergy will lead to the main goals of the project. The project will consist of three main objectives including synthesis and structural characterization of benzazole derivatives, computational research and biological evaluation. Within the project synthesis of small library of benzazole derivatives will be performed while additionally this collaborative research should result in the optimization of the benzazole scaffold which will ensure more efficient activity and optimized properties of lead compounds as antioxidants and antitumor agents. Computational chemistry and QSAR modelling will allow a structural optimization of chosen lead compounds. Biological evaluation will include in vitro assays for evaluation of antioxidative activity. Additionally, the chosen compounds will be tested for antitproliferative activity in vitro on human cancer cells. To get more insight into the mechanisms of action of lead compounds the assessment of ROS levels in the cells as well in mitochondria, along with the oxidative DNA damage and analysis of expression of proteins will be performed. One of the objectives will be the development of less toxic derivatives as potential fluorescent probes for detection of biomacromolecules. Finally, the presented research is based on joint research of different institutions including researchers from different scientific fields. Proposed project is based on the research in the field of medicinal chemistry with focus on possible further target research as well as further development of our scientific group on the international level.