Abstract
Synthesis of ( 2R)-2-carboxymethyl-3-(4-(phosphonomethyl)phenyl) proprionic acid ( 5) in tert-butyl-protected form ( 6) and its use for the preparation of a Grb2 SH2 domain-directed tripeptide ( 8a) is reported. In extracellular ELISA-based assays, 8a exhibits potent Grb2 SH2 domain binding affinity (IC 50=8 nM). Against cultures of MDA-MB-453 breast cancer cells, which over-express erbB-2 tyrosine kinase, 8a is also antimitogenic at concentrations equivalent to those required to inhibit intracellular association of Grb2 protein with phosphorylated p185 erbB-2 protein (IC 50=8 μM). Analogue 6 may be useful for the preparation of a variety of phosphatase-stable SH2 domain-directed ligands.
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