Our patent reports on the analogues of 1,3-bis(4-nitrophenyl)triazenes, their pharmaceutically acceptable salts and N-acyl derivatives as new agents for the treatment of different types of tumors. The described compounds show cytotoxicity at very low concentrations. They are in fact 4-nitro-1,3-diaryltriazenes that possess two additional electron-withdrawing groups and are highly cytotoxic compounds. Their acylation at the triazene nitrogen increases the solubility. Furthermore, N-acyltriazenes can be considered as prodrugs of their non-acylated analogues. The antiproliferative activity of new compounds also depends on the type of the substituent introduced at the ortho position of the two benzene rings. It turned out that trifluoromethyl substituent increased cytotoxicity of the compound more than other groups.
F.32 International patent
COBISS.SI-ID: 30639621In the frame of the working group in COST D24 and in an informal cooperation within COST D40 we were developing different methods of catalysis, which had been previously shown to be industrially important; for example heterogeneous catalytic hydrogenation of dehydroamino acids. As a team of four authors from three countries, we described general development in the field of dehydroamino acids and bicyclooctenes with the emphasis on our joint results. The book was issued as a conclusion of the action COST D40, the editor was P. G. Andersson as a coordinator of one of the working groups.
D.06 Final report on a foreign/international project
COBISS.SI-ID: 35934469On invitation from the editorial board, J. Košmrlj as a Volume Editor prepared book entitled ’Click Triazoles’, published within the Springer series Topics in Heterocyclic Chemistry. This invitation is recognition to our research work in the field of heterocyclic chemistry. Additional recognition and acknowledgement is demonstrated by positive reply of leading scientists in the field to contribute their chapters. These include: 1) Semin Lee, Amar H. Flood, Indiana University, Bloomington, USA. Binding Anions in Rigid and Reconfigurable Triazole Receptors. 2) Hak-Fun Chow, Chui-Man Lo, and Yuan Chen, Center of Novel Functional Molecules, and Institute of Molecular Functional Materials and The Chinese University of Hong Kong, China. Triazole-Based Polymer Gels. 3) James D. Crowley and David A. McMorran, University of Otago, New Zealand. "Click-triazole" coordination chemistry: Exploiting 1,4-disubstituted-1,2,3-triazoles as ligands. 4) S. Mignani, Y. Zhou, T. Lecourt, L. Micouin, Université Paris Descartes, France. Recent developments in the synthesis 1,4,5-trisubstituted triazoles. 5) Michael Watkinson, Queen Mary University of London, UK. Click triazoles as chemosensors. 6) Tianqing Zheng, Sara Rouhanifard, Abubakar Jalloh, Peng Wu, Albert Einstein College of Medicine, Yeshiva University, USA. Click Triazoles for Bioconjugation. 7) Benjamin R. Buckley and Harry Heaney, Loughborough University, UK. Mechanistic Investigations of Copper(I) Catalysed Alkyne-Azide Cycloaddition Reactions.
C.01 Editorial board of a foreign/international collection of papers/book
COBISS.SI-ID: 36164101In the frame of the invited lecture at the important international conference the versatility of 2H-pyran-2-ones as starting compounds for a wide array of Diels–Alder reactions was presented. With a high regio- and stereoselectivity the synthesis of derivatives of aniline, bi- and terphenyl systems, indoles, isoindoles, bicyclo/2.2.2/octenes and 7-oxabicyclo/2.2.2/octene is enabled. The transformations presented were investigated under thermal conditions (conventional and microwave heating) and high pressure (13 kbar). The application of suitable organocatalysts (such as DABCO) or dehydrogenation catalysts (such as Darco KB) in some cases even increased the scope of these transformations. The last case is especially instructive as it shows how Darco KB can represent an ecologically more acceptable (and cheaper) alternative to the precious metals (on active charcoal as solid support) otherwise used in such reactions.
B.04 Guest lecture
COBISS.SI-ID: 35848197The state-of-the art of asymmetric hydrogenation and transfer hydrogenation of ketones leading to optically active alcohols, on both laboratory and industrial scales is described. The examples of the use of homogenous and heterogeneous metal catalysts approaching enzymatic performance with respect to activity and selectivity in some cases are given. Concerning the environmental and economic issues, the introduction of less-toxic metal catalysts like iron and copper is highly desirable. Hydrogenation reactions are also feasible in aqueous medium by choosing appropriate catalyst systems.
F.30 Professional assessment of the situation
COBISS.SI-ID: 36250117