Piperazinediones also known as diketopiperazines, are the smallest cyclic peptides, as well as a common motif in several natural products with therapeutic properties.'It has been shown that bisdiketopiperazines exhibit antitumor activity against Lewis lung carcinoma, sarcoma 180, L12 10 leukemia, P388 leukemia, B 16 myeloma, malignant lymphoma, C-26 colon, C- 38 human colon and breast cancer. 2-8 They have also been used in clinical trial ...