Macrocycles were designed to antagonize the protein-protein interaction p53-MDM2 based on the three-finger pharmacophore FWL. The synthesis was accomplished by a rapid, one-pot synthesis of indole-based macrocycles based on Ugi macrocyclization. The reaction of 12 different α,ω-amino acids and different indole-3-carboxaldehyde derivatives afforded a unique library of macrocycles otherwise difficult to access. Screening of the library for p53-MDM2 inhibition by fluorescence polarization and H,N HSQC NMR measurements confirm MDM2 binding.
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| http://dx.doi.org/10.3762/bjoc.15.45 | DOI Listing |
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