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Chemical Compound Review

ICRF-161     4-[3-(3,5-dioxopiperazin-1...

Synonyms: SureCN9752550, CHEBI:50231, AC1L3GPM, A815326, 35259-82-6, ...
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Disease relevance of ICRF 159


High impact information on ICRF 159


Chemical compound and disease context of ICRF 159


Biological context of ICRF 159


Anatomical context of ICRF 159

  • In contrast, 24-hr incubation of human lymphocytes with up to 50 micrograms ICRF 159 per ml had no effect on their viability or on their ability to be stimulated by phytohemagglutinin [3].
  • CHO cell colony formation was inhibited by 50% following either an 8.5-hr exposure of exponentially growing cells to 10 micrograms ICRF 159 per ml or a 24-hr exposure to 3 micrograms ICRF 159 per ml [3].
  • The cytokinetic and cytotoxic effects of ICRF-159 and ICRF-187 in vitro and ICRF-187 in human bone marrow in vivo [17].
  • It appears that adequate surgery together with rapid radiation therapy in combination with razoxane, a radiosensitizer and agent that can normalize tumor blood vessels, is able to improve the local control rate and thus perhaps to alter the natural history of this disease [18].
  • The effects of razoxane (ICRF 159) on the production of collagenase and inhibitor (TIMP) by stimulated rabbit articular chondrocytes [19].

Associations of ICRF 159 with other chemical compounds


Gene context of ICRF 159


Analytical, diagnostic and therapeutic context of ICRF 159


  1. Razoxane (ICRF 159) in psoriasis. Atherton, D.J., Wells, R.S., Hellman, K. Lancet (1976) [Pubmed]
  2. Enhancement of experimental lung metastases by cultured B16 melanoma cells treated with (+/-)-1,2-bis(3,5-dioxopiperazin-1-y)propane (ICRF-159). Lazo, J.S., Ingber, D.E., Sartorelli, A.C. Cancer Res. (1978) [Pubmed]
  3. Effects of the L isomer (+)-1,2-bis(3,5-dioxopiperazine-1-yl)propane on cell survival and cell cycle progression of cultured mammalian cells. Traganos, F., Darzynkiewicz, Z., Melamed, M.R. Cancer Res. (1981) [Pubmed]
  4. A phase II study of razoxane, an antiangiogenic topoisomerase II inhibitor, in renal cell cancer with assessment of potential surrogate markers of angiogenesis. Braybrooke, J.P., O'Byrne, K.J., Propper, D.J., Blann, A., Saunders, M., Dobbs, N., Han, C., Woodhull, J., Mitchell, K., Crew, J., Smith, K., Stephens, R., Ganesan, T.S., Talbot, D.C., Harris, A.L. Clin. Cancer Res. (2000) [Pubmed]
  5. Soluble Tie2 and Flt1 extracellular domains in serum of patients with renal cancer and response to antiangiogenic therapy. Harris, A.L., Reusch, P., Barleon, B., Hang, C., Dobbs, N., Marme, D. Clin. Cancer Res. (2001) [Pubmed]
  6. Phase II study: treatment of non-Hodgkin's lymphoma with an oral antitumor derivative of bis(2,6-dioxopiperazine). Ohno, R., Yamada, K., Hirano, M., Shirakawa, S., Tanaka, M., Oguri, T., Kodera, Y., Mitomo, Y., Ikeda, Y., Yokomaku, S. J. Natl. Cancer Inst. (1992) [Pubmed]
  7. Inheritance of cellular resistance to the antitumor agent ICRF 159 in somatic cell hybrids. Edgar, D.H., Creighton, A.M. J. Natl. Cancer Inst. (1982) [Pubmed]
  8. Methotrexate in lieu of razoxane for incapacitating psoriasis. Steinman, H.K., Griffiths, W.A., Levene, G.M. Lancet (1984) [Pubmed]
  9. "Vasocrine" formation of tumor cell-lined vascular spaces: implications for rational design of antiangiogenic therapies. Rybak, S.M., Sanovich, E., Hollingshead, M.G., Borgel, S.D., Newton, D.L., Melillo, G., Kong, D., Kaur, G., Sausville, E.A. Cancer Res. (2003) [Pubmed]
  10. DNA topoisomerase II is the molecular target of bisdioxopiperazine derivatives ICRF-159 and ICRF-193 in Saccharomyces cerevisiae. Ishida, R., Hamatake, M., Wasserman, R.A., Nitiss, J.L., Wang, J.C., Andoh, T. Cancer Res. (1995) [Pubmed]
  11. Suppression of metastatic potential and up-regulation of gelatinases and uPA in LLC by protracted in vivo treatment with dacarbazine or razoxane. Garbisa, S., Onisto, M., Peron, A., Perissin, L., Rapozzi, V., Zorzet, S., Giraldi, T. Int. J. Cancer (1997) [Pubmed]
  12. Combination chemotherapy of advanced colorectal cancer with triazinate and ICRF-159 after failure of 5-Fluorouracil. Vogl, S.E., Lanham, R., Kaplan, B.H. Oncology (1980) [Pubmed]
  13. The mutagenic potency of 4 agents at the thymidine kinase locus in mouse lymphoma L5178Y cells in vitro: effects of exposure time. Edgar, D.H. Mutat. Res. (1985) [Pubmed]
  14. Therapy-related acute nonlymphocytic leukemia with inversion of chromosome 16 and a sustained remission. Baglin, T.P., Galvin, G.P., Pollock, A. Cancer Genet. Cytogenet. (1987) [Pubmed]
  15. dl-N,N'-dicarboxamidomethyl-N,N'-dicarboxymethyl-1,2-diaminopropane (ICRF-198) and d-1,2-bis(3,5-dioxopiperazine-1-yl)propane (ICRF-187) inhibition of Fe3+ reduction, lipid peroxidation, and CaATPase inactivation in heart microsomes exposed to adriamycin. Vile, G.F., Winterbourn, C.C. Cancer Res. (1990) [Pubmed]
  16. Biologic mechanisms for the regulation of normal human keratinocyte proliferation and differentiation. Wilke, M.S., Hsu, B.M., Wille, J.J., Pittelkow, M.R., Scott, R.E. Am. J. Pathol. (1988) [Pubmed]
  17. The cytokinetic and cytotoxic effects of ICRF-159 and ICRF-187 in vitro and ICRF-187 in human bone marrow in vivo. Wheeler, R.H., Clauw, D.J., Natale, R.B., Ruddon, R.W. Investigational new drugs. (1983) [Pubmed]
  18. Treatment options for malignant hemangioendotheliomas of the thyroid. Rhomberg, W., Boehler, F., Eiter, H., Fritzsche, H., Breitfellner, G. Int. J. Radiat. Oncol. Biol. Phys. (2004) [Pubmed]
  19. The effects of razoxane (ICRF 159) on the production of collagenase and inhibitor (TIMP) by stimulated rabbit articular chondrocytes. Duncan, S.J., Reynolds, J.J. Biochem. Pharmacol. (1983) [Pubmed]
  20. Inhibition of topoisomerase II by antitumor agents bis(2,6-dioxopiperazine) derivatives. Tanabe, K., Ikegami, Y., Ishida, R., Andoh, T. Cancer Res. (1991) [Pubmed]
  21. Cytoprotective agents for anthracyclines. Dorr, R.T. Semin. Oncol. (1996) [Pubmed]
  22. Inhibition of collagen peptidase in HeLa cells and human tumours by compounds including drugs used in cancer therapy. Boggust, W.A., McGauley, H. Br. J. Cancer (1978) [Pubmed]
  23. Interaction of radiation and AT 1727 in HeLa S-3 cells in culture. He, S.Q., Kim, S.H., Kim, J.H. Int. J. Radiat. Oncol. Biol. Phys. (1985) [Pubmed]
  24. Analysis of a core domain in Drosophila DNA topoisomerase II. Targeting of an antitumor agent ICRF-159. Chang, S., Hu, T., Hsieh, T.S. J. Biol. Chem. (1998) [Pubmed]
  25. Stable induction of c-jun mRNA expression in normal human keratinocytes by agents that induce predifferentiation growth arrest. Blatti, S.P., Scott, R.E. Cell Growth Differ. (1992) [Pubmed]
  26. Response to ICRF-159 in cell lines resistant to cleavable complex-forming topoisomerase II inhibitors. Davies, S.L., Bergh, J., Harris, A.L., Hickson, I.D. Br. J. Cancer (1997) [Pubmed]
  27. Two functionally distinct classes of growth arrest states in human prokeratinocytes that regulate clonogenic potential. Pittelkow, M.R., Wille, J.J., Scott, R.E. J. Invest. Dermatol. (1986) [Pubmed]
  28. ICRF 159 plus radiation versus radiation therapy alone in cervical carcinoma. A double-blind study. Belloni, C., Mangioni, C., Bortolozzi, G., Carinelli, S., D'Incalci, M., Maggioni, A., Morasca, L. Oncology (1983) [Pubmed]
  29. Clinical trial of combination chemotherapy and specific active immunotherapy in disseminated melanoma. Newlands, E.S., Oon, C.J., Roberts, J.T., Elliott, P., Mould, R.F., Topham, C., Madden, F.J., Newton, K.A., Westbury, G. Br. J. Cancer (1976) [Pubmed]
  30. Effect of surgery and adjuvant chemotherapy on the R3327 MAT-Ly Lu tumor. Kadmon, D., Heston, W.D., Fair, W.R. Prostate (1981) [Pubmed]
  31. Measurement of renal tumour and normal tissue perfusion using positron emission tomography in a phase II clinical trial of razoxane. Anderson, H., Yap, J.T., Wells, P., Miller, M.P., Propper, D., Price, P., Harris, A.L. Br. J. Cancer (2003) [Pubmed]
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