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Tröger's base scaffold in racemic and chiral fashion as a spacer for bisdistamycin formation. Synthesis and DNA binding study |
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| Authors: | Martin Valí k,Luká &scaron Palivec,Marcela Tkadlecová ,Viktor Brabec |
| Affiliation: | a Institute of Chemical Technology Prague, Dept. of Analytical Chemistry, Technická 5, 166 28 Prague 6, Czech Republic b Institute of Biophysics, Academy of Sciences of the Czech Republic, Královopolská 135, 612 65 Brno, Czech Republic c Institute of Chemical Technology Prague, Dept. of Physics and Measurements, Technická 5, 166 28 Prague 6, Czech Republic |
| Abstract: | ‘Head-to-head’ oligo-N-methylpyrrole peptide dimers linked by a methano[1,5]diazocin scaffold are presented in racemic as well as chiral fashion. Their DNA binding activities were assayed on calf thymus DNA, poly(dA-dT)2, and poly(dC-dG)2 by NMR and ECD spectroscopies, and fluorescence probe displacement assay. The presented dimers prefer AT sequences, but show higher affinity to poly(dC-dG)2 than distamycin A. The (4R,9R) configuration of methanodiazocin bridge was found to be better suited for interaction with ct-DNA and poly(dA-dT)2 than (4S,9S) configuration. |
| Keywords: | Trö ger's base Distamycin dimer Enantioselective binding Dissymmetry factor VCD |
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