Design, synthesis, and evaluation of potent and selective benzoyleneurea-based inhibitors of protein geranylgeranyltransferase-I

Using a benzoyleneurea scaffold as a mimetic for the central dipeptide (AA), CAAX peptidomimetic inhibitors that selectively block the activity of PGGTase-I over PFTase were synthesized. In this series, compound 6c containing a L-phenylalanine moiety displayed the highest inhibition activity against...

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