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

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

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4 Boron clusters puncture lipid membranes Current (pA) 13 14 15 16 17 0.25 μM B 12 I 12 -100mV constant

5 Boron cluster compounds can be enzyme inhibitors and receptor ligands

6 Brynda et al., Angew. Chem. Int. Ed. 51, 13760–13763, 2013 compoundCA IX (µM) o0.38 m1.12 nido5.09 CB 11 2.20 Carbonic Anhydrase IX

7 Lee et al., J. Med. Chem. 2012, 55, 7290−7294 Inhibitor of nicotinamide phosphoribosyltranferase compoundA549DLD1T47D FK8661.623.143.20 o0.921.691.29 m0.410.310.32 p0.992.200.58 Inhibition of cell growth IC50 (nM)

8 compoundCOX1COX2 indomethacin methyl ester>250.250 o12.80.084 m>25 p Scholz et al., Bioorg Med Chem 20, 4830–4837, 2012 IC50 values of cyclic oxygenases (µM) indomethacin methyl ester

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

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

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13 Dihydrogen bonds between dodecaborate and water

14 Ural, Assaf, Nau γ-Cyclodextrin

15 Ural, Assaf, Nau

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

18 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

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