Regiospecific and conformationally restrained analogs of melphalan and dl-2-NAM-7 and their affinities for the large neutral amino acid transporter (system LAT1) of the blood-brain barrier

Placing the mustard moiety at C-7 of the tetralin ring (5c) affords greatest affinity for the System LAT1 transporter; the more conformationally restrained analogs (6 and 7) of DL-2-NAM-7 had lower affinity than 5c.