An important socio-economically relevant result is successfully accomplished doctoral study of young researcher Martin Gazvoda as he was awarded for his PhD Thesis by the Krka Award in October 2013 [COBISS.SI-ID 1644591]). After PhD study Dr. Gazvoda was granted by a post-doctoral project that was assigned to him from the European Funds. Currently, he is working on this project. Within his PhD Thesis Martin Gazvoda designed several new 2,3-diarylpropenoic acids that were synthesized and evaluated as inhibitors of AKR1C1-AKR1C3. A modification of the structure revealed that the 4-methylsulfonylphenyl substituent at the position 2 of the 2,3-diarylpropenoic acid is an appropriate one to obtain a selective inhibition of AKR1C3. Two of the analogs, bearing 4-methylphenyl and 4-ethylphenyl groups at the position 3 are the most selective ones. They practically do not inhibit AKR1C1 and AKR1C2 at a 100 µM concentration and may serve as a good starting point for the development of new antitumor agents. He also developed a general, mild and selective synthesis for N-sulfonylformamidines from sulfonamides or N-acylated sulfonamides. He applied Vilsmeier reagent obtained in situ from N,N-disubstituted formamides and oxalyl chloride. Optically active substrates did not racemize during the process. The efficient and mild cleavage of N-sulfonylformamidines can be achieved with hydrazine hydrate in ethanol. The entire procedure constitutes a simple method for protecting and deprotecting of the sulfonamide moiety. The research covered by his PhD Thesis was published in Eur. J. Med. Chem. and in Eur. J. Org. Chem., and one manuscript is under preparation.
D.09 Tutoring for postgraduate students
COBISS.SI-ID: 36736517Recognition of our highly successful long term academic and applicative-industrial activities in synthetic organic methodologies, including the field of biologically relevant compounds, was the invitation of Sandoz GmbH, Kundl, Austria in 2013 to collaborate on some of their research projects. This invitation was also motivated by a large number of successfully completed projects between our group and Lek-Sandoz, Slovenia in previous years. With no doubt, the invitation of a world leader in pharmaceuticals is a relevant international survey of a technological level and potentials in applicative implementation of a programme (See also 12).
F.17 Transfer of existing technologies, know-how, methods and procedures into practice
COBISS.SI-ID: 1686063In 2013 the Slovenian Research Agency recognized our contribution published in Proceedings of the National Academy of Sciences USA as an outstanding result in 2012. The publication is the result of research collaboration between the research groups at the Faculty of Chemistry and Chemical Technology of the University of Ljubljana and the Department of Pharmacology of the David Geffen School of Medicine of the University of California at Los Angeles. In the publication we described new development in the field of molecular probes for detection of changes in the brain of patients with some neurodegenerative diseases. The original breakthrough was achieved when we discovered compound dubbed as FDDNP. It enabled the development of the first non-destructive method for the diagnosis of Alzheimer's disease in living patients. We successfully publish and transfer the results of our ongoing research in the field into practice.
F.22 Improvement to existing health/diagnostic methods/procedures
COBISS.SI-ID: 1685551