Merbarone
Merbarone structure
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Common Name | Merbarone | ||
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| CAS Number | 97534-21-9 | Molecular Weight | 263.27200 | |
| Density | 1.51g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C11H9N3O3S | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
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Dominant lethal mutations of topoisomerase II inhibitors etoposide and merbarone in male mice: a mechanistic study.
Arch. Toxicol. 86(5) , 725-31, (2012) Two topoisomerase II inhibitors, etoposide and merbarone, were tested for the induction of dominant lethal mutations in male mice. Etoposide was administered at a dosage of 30 or 60 mg/kg. Merbarone was administered at a dosage of 40 or 80 mg/kg. These males ... |
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Merbarone: an antitumor agent entering clinical trials.
Invest. New Drugs 5(2) , 137-43, (1987) Merbarone was developed to clinical trial stage on the basis of its 'curative' activity against P388 and L1210 leukemias and moderate activity against B16 melanoma and M5076 sarcoma. Its activity appears to be schedule-dependent favoring a longer duration of ... |
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Differential cell cycle-specificity for chromosomal damage induced by merbarone and etoposide in V79 cells.
Mutat. Res. 616(1-2) , 70-82, (2007) Merbarone, a topoisomerase II (topo II) inhibitor which, in contrast to etoposide, does not stabilize topo II-DNA cleavable complexes, was previously shown to be a potent clastogen in vitro and in vivo. To investigate the possible mechanisms, we compared the ... |
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Novel mechanisms of resistance to inhibitors of DNA topoisomerases.
Adv. Enzyme Regul. 37 , 17-26, (1997)
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Merbarone induces activation of caspase-activated DNase and excision of chromosomal DNA loops from the nuclear matrix.
Mol. Pharmacol. 69(4) , 1477-85, (2006) Studies were carried out to address possible cellular mechanisms by which merbarone, a catalytic inhibitor of DNA topoisomerase II, can block tumor cell growth without inducing extensive DNA cleavage. Merbarone induced the release of high molecular weight DNA... |
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Synthesis and antiproliferative activity of basic thioanalogues of merbarone.
Bioorg. Med. Chem. 11(12) , 2575-89, (2003) Three series of 5-substituted 1,3-diphenyl-6-(omega-dialkyl- and omega-cyclo-aminoalkyl)thio-2-thiobarbiturates (11-13) were synthesized as polysubstituted thioanalogues of merbarone, a topoisomerase II inhibitor acting on the catalytic site. To better unders... |
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The DNA topoisomerase II catalytic inhibitor merbarone is genotoxic and induces endoreduplication.
Mutat. Res. 738-739 , 45-51, (2012) In the last years a number of reports have shown that the so-called topoisomerase II (topo II) catalytic inhibitors are able to induce DNA and chromosome damage, an unexpected result taking into account that they do not stabilize topo II-DNA cleavable complex... |
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DNA cleavage and Trp53 differentially affect SINE transcription.
Genes Chromosomes Cancer 46(3) , 248-60, (2007) Among the cellular responses observed following treatment with DNA-damaging agents is the activation of Short Interspersed Elements (SINEs; retrotransposable genetic elements that comprise over 10% of the human genome). By placing a human SINE (the Alu elemen... |
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Interference with topoisomerase IIalpha potentiates melphalan cytotoxicity.
Int. J. Oncol. 20(2) , 311-8, (2002) We studied the consequences of interfering with DNA topoisomerase IIalpha (topo IIalpha) activity on melphalan-induced cytotoxicity. In order to accomplish our goal we used three different approaches to interfere with topo IIalpha. These include: i) use of th... |
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Phase II trial of merbarone in patients with malignant brain tumors.
Med. Oncol. 14(3-4) , 159-62, (1997) The standard treatment for patients with primary malignant glioma includes surgical resection, radiotherapy, and nitrosourea. Despite this multimodality approach, adults with newly diagnosed glioblastoma multiforme (GBM) and high-grade astrocytoma have a medi... |