Solid-phase synthesis of symmetrical 3,6-bispeptide-acridone conjugates
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Published on: October 2, 2018
Sylvain Ladame1, R John Harrison, Stephen Neidle
1University Chemical Laboratory, University of Cambridge, Lensfield Road, Cambridge CB2 1EW, UK.
Abstract:
[reaction: see text] A novel high-yielding method for the solid-phase synthesis of 3,6-bispeptide-acridone conjugates is reported. It involves initial coupling of bifunctionalized acridone to a resin-bound peptide followed by an on-bead site-site reaction to couple the second peptide. This method leads to clean symmetrical bispeptide derivatives and appears to be general. This strategy will enable the generation of a library of 3,6-bispeptide-acridones to be screened for selective binding to telomeric G-quadruplex DNA.

