Welcome to Jacobs University Bremen Presenter Name | Meeting | Date Boron clusters as boron carriers for BNCT: Possibilities and problems Detlef Gabel.

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Presentation transcript:

Welcome to Jacobs University Bremen Presenter Name | Meeting | Date Boron clusters as boron carriers for BNCT: Possibilities and problems Detlef Gabel Jacobs University Bremen

Boron clusters puncture lipid membranes Current (pA) μM B 12 I mV constant

Boron cluster compounds can be enzyme inhibitors and receptor ligands

Brynda et al., Angew. Chem. Int. Ed. 51, 13760–13763, 2013 compoundCA IX (µM) o0.38 m1.12 nido5.09 CB Carbonic Anhydrase IX

Lee et al., J. Med. Chem. 2012, 55, 7290−7294 Inhibitor of nicotinamide phosphoribosyltranferase compoundA549DLD1T47D FK o m p Inhibition of cell growth IC50 (nM)

compoundCOX1COX2 indomethacin methyl ester> o m>25 p Scholz et al., Bioorg Med Chem 20, 4830–4837, 2012 IC50 values of cyclic oxygenases (µM) indomethacin methyl ester

Fan et al, J Chromatogr A 1256, 98, 2012

Karki et al., Inorg Chem 51, 4894, 2012

Dihydrogen bonds between dodecaborate and water

Ural, Assaf, Nau γ-Cyclodextrin

Ural, Assaf, Nau

Association constants of boron clusters with γ-cyclodextrin Ural, Assaf, Nau

Boron clusters can interact strongly with lipids proteins carbohydrates Interactions cannot be predicted easily Unwanted behavior cannot be excluded Can one use the interaction for other purposes? In vitro and in vivo testing appears necessary