Synonyms: Amplimexon® (proposed trade name) | BM 06002 | BM-06002
Compound class:
Synthetic organic
Comment: Imexon is a cyclizised 2-cyanoaziridine compound being investigated as an antitumour agent [4-5]. 2-cyanoaziridine compounds bind thiols such as cysteine, depleting them and allowing the accumulation of reactive oxygen species. This effect activates antioxidant gene expression, signifying induction of an oxidative stress response [1] and leads to irreversible cell damage and apoptosis.
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References |
1. Baker AF, Landowski T, Dorr R, Tate WR, Gard JM, Tavenner BE, Dragovich T, Coon A, Powis G. (2007)
The antitumor agent imexon activates antioxidant gene expression: evidence for an oxidative stress response. Clin Cancer Res, 13 (11): 3388-94. [PMID:17545547] |
2. Dvorakova K, Payne CM, Tome ME, Briehl MM, McClure T, Dorr RT. (2000)
Induction of oxidative stress and apoptosis in myeloma cells by the aziridine-containing agent imexon. Biochem Pharmacol, 60 (6): 749-58. [PMID:10930529] |
3. Engel RH, Evens AM. (2006)
Oxidative stress and apoptosis: a new treatment paradigm in cancer. Front Biosci, 11: 300-12. [PMID:16146732] |
4. Hersh EM, Gschwind CR, Taylor CW, Dorr RT, Taetle R, Salmon SE. (1992)
Antiproliferative and antitumor activity of the 2-cyanoaziridine compound imexon on tumor cell lines and fresh tumor cells in vitro. J Natl Cancer Inst, 84 (16): 1238-44. [PMID:1640482] |
5. Remers WA, Dorr RT. (2012)
Chemistry and pharmacology of imexon and related cyanoaziridines. Curr Med Chem, 19 (33): 5745-53. [PMID:22998528] |
6. Wondrak GT. (2009)
Redox-directed cancer therapeutics: molecular mechanisms and opportunities. Antioxid Redox Signal, 11 (12): 3013-69. [PMID:19496700] |