A facile synthesis of four distamycin analogues that bear the dansyl fluorophore is described. The nature of the linkage between the fluorophore and the sequence recognition element had a dramatic effect on the fluorescence properties of these ligands upon DNA binding.
Novel distamycin analogues: facile synthesis of cholesterol conjugates of distamycin-like oligopeptides
✍ Scribed by Santanu Bhattacharya; Mini Thomas
- Publisher
- Elsevier Science
- Year
- 2001
- Tongue
- French
- Weight
- 112 KB
- Volume
- 42
- Category
- Article
- ISSN
- 0040-4039
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## Abstract The ^1^H and ^13^C NMR resonances for a novel distamycin conjugate, 3‐[1‐methyl‐4‐[1‐methyl‐4‐[1‐methyl‐4‐[N^1^‐[5‐methyl‐2,4(1__H__,3__H__)pyrimidinedione]acetylamino]pyrrole‐2‐carboxamido]pyrrole‐2‐carboxamido]pyrrole‐2‐carboxamido]propionamidine hydrochloride (**1**), were assigned,
The ®rst examples of distamycin analogs, which lack hydrogen bond interactor groups at the N-terminus, have been synthesized. The bispyrrole peptide did not exhibit any detectable binding with double-stranded (ds) DNA. However, all other homologues did bind to ds-DNA strongly, with the binding aniti