Antitumor activity of MST-16, a novel derivative of bis(2,6-dioxopiperazine), in murine tumor models.

Abstract

We studied the antitumor activity of newly synthesized bis(1-acyloxymethyl) derivatives of 4,4'-(1,2-ethanediyl)bis(2,6-piperazinedione) using i.p.-i.p. models of P388 leukemia and B16 myeloma. As a result, we found 4,4'-(1,2-ethanediyl)bis(1-isobutoxycarbonyloxymethyl-2,6-piperazi nedione) (MST-16) to possess considerable therapeutic activity. MST-16 showed not only marked life-prolonging effects in both P388 leukemia- and B16 melanoma-bearing mice but also a greater therapeutic ratio than did its parent compounds, ICRF-154 and ICRF-159. Further studies revealed that MST-16 has considerable therapeutic activity against a number of other tumors such as ascitic forms of L1210 leukemia, colon 26 adenocarcinoma, and MH-134 hepatoma and solid forms of B16 melanoma, Lewis lung carcinoma, colon 38 adenocarcinoma, and M5076 fibrosarcoma. These results suggest that MST-16 is very promising as an antitumor agent.

• Authors: T Narita, S Yaguchi, T Komatsu, M Takase, A Hoshino, M Inaba, S Tsukagoshi
• Journal: Cancer chemotherapy and pharmacology (Cancer Chemother Pharmacol) Vol. 26 Issue 3 Pg. 193-7 ( 1990) ISSN: 0344-5704 [Print] Germany
• PMID: 2357766 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Antineoplastic Agents
• Piperazines
• Razoxane
• 1,2-bis(3,5-dioxopiperazin-1-yl)ethane
• sobuzoxane

Topics

• Animals
• Antineoplastic Agents (therapeutic use)
• Drug Screening Assays, Antitumor
• Leukemia P388 (drug therapy)
• Leukemia, Experimental (drug therapy)
• Melanoma, Experimental (drug therapy)
• Mice
• Mice, Inbred Strains
• Neoplasm Transplantation
• Piperazines (therapeutic use)
• Razoxane (analogs & derivatives, therapeutic use)
• Structure-Activity Relationship
• Tumor Cells, Cultured (drug effects)