Abstract: In a previous paper we reported the preparation of derivatives of N-phthalylglutamine as well as their inhibitory activities against glutaminase and anticancer actions. In order to study the relationship between chemical structures and biological activities so as to search for better anticancer agents, twenty-four compounds with different structures such as a-phthalimido glutaric acid γ-amides of aromatic amines, substituted-α-phthalimido-γ-glutaramides ortho-carboxy-benzamido and metao or para-carboxy sulfonamido glutaric acid derivatives and also α-succinyl glutamine were prepared. The detailed biological studies were reported in Acta Biochimica et Biophysica Sinica.