Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 19, Issue 7, Pages 2442-2449Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.201203005
Keywords
inhibitors; peptide mimetics; proteinprotein interactions; Suzuki coupling; teraryl
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Funding
- Volkswagenstiftung, Hannover
- PLACEBO (Platform for Chemical Biology) project, Austrian Genome Project GEN-AU
- Forschungsforderungsgesellschaft (FFG)
- Bundesministerium fur Wissenschaft und Forschung (BMWF)
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Teraryl-based -helix mimetics have proven to be useful compounds for the inhibition of proteinprotein interactions (PPI). We have developed a modular and flexible approach for the synthesis of teraryl-based -helix mimetics. Central to our strategy is the use of a benzene core unit featuring two leaving groups of differentiated reactivity in the Pd-catalyzed cross-coupling used for terphenyl assembly. With the halogen/diazonium route and the halogen/triflate route, two strategies have successfully been established. The synthesis of core building blocks with aliphatic (Ala, Val, Leu, Ile), aromatic (Phe), polar (Cys, Lys), hydrophilic (Ser, Gln), and acidic (Glu) amino acid side chains are reported.
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