The preparation of a series of synthetic sulfur-containing amino acids is described. These compounds included heterocyclic analogues of L-cysteine, DL-norcysteine, and DL-homocysteine. The amino acids were assessed for their ability to inhibit the neutral amino acid transport systems of the Sarcoma 37 ascites tumor cell and their inhibitions were compared with those of L-methionine and L-ethionine. Transport studies indicated that the amino acids synthesized were capable of inhibiting the uptake of [3H]-L-histidine in the S37 cell.