A series of novel 3-aryl-4-oxo-thiazolidin-2-carboxylic acid amides were synthesized and evaluated for their antiproliferative activity for three tumor cells. Some compounds showed weak cytotoxicity against A-549 and Hela tumor cells, but no antiproliferative activity against BGC-823, which suggested such compounds with a certain cytotoxicity selectivity to the three tumor cells. Among them, compound 7ad was the best one against A-549 with the IC₅₀ value of 21.0 μmol•L^－1, nearly equivalent to that of the positive control cisplatin (IC₅₀＝19.4 μmol•L^－1). Preliminary structure activity relationship analysis of these analogues suggested that the steric factor may be important to the anti-tumor activity.

Key words: thiazolidin-4-one, synthesis, cytotoxic activity, tumor cell, structure-activity relationship