Triapine
Triapine structure
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Common Name | Triapine | ||
|---|---|---|---|---|
| CAS Number | 143621-35-6 | Molecular Weight | 195.245 | |
| Density | 1.5±0.1 g/cm3 | Boiling Point | 436.0±55.0 °C at 760 mmHg | |
| Molecular Formula | C7H9N5S | Melting Point | 234°C(lit.) | |
| MSDS | Chinese USA | Flash Point | 217.5±31.5 °C | |
| Symbol |
GHS06 |
Signal Word | Danger | |
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Trypanotoxic activity of thiosemicarbazone iron chelators.
Exp. Parasitol. 150 , 7-12, (2015) Only a few drugs are available for treating sleeping sickness and nagana disease; parasitic infections caused by protozoans of the genus Trypanosoma in sub-Saharan Africa. There is an urgent need for the development of new medicines for chemotherapy of these ... |
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Iron-targeting antitumor activity of gallium compounds and novel insights into triapine(®)-metal complexes.
Antioxid. Redox Signal. 18(8) , 956-72, (2013) Despite advances made in the treatment of cancer, a significant number of patients succumb to this disease every year. Hence, there is a great need to develop new anticancer agents.Emerging data show that malignant cells have a greater requirement for iron th... |
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Vacuolar-ATPase Inhibition Blocks Iron Metabolism to Mediate Therapeutic Effects in Breast Cancer.
Cancer Res. 75 , 2863-74, (2015) Generalized strategies to improve breast cancer treatment remain of interest to develop. In this study, we offer preclinical evidence of an important metabolic mechanism underlying the antitumor activity of inhibitors of the vacuolar-type ATPase (V-ATPase), a... |
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Ribonucleotide reductase inhibition enhances chemoradiosensitivity of human cervical cancers.
Radiat. Res. 174(5) , 574-81, (2010) For repair of damaged DNA, cells increase de novo synthesis of deoxyribonucleotide triphosphates through the rate-limiting, p53-regulated ribonucleotide reductase (RNR) enzyme. In this study we investigated whether pharmacological inhibition of RNR by 3-amino... |
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Deoxynucleoside salvage facilitates DNA repair during ribonucleotide reductase blockade in human cervical cancers.
Radiat. Res. 176(4) , 425-33, (2011) Cells generate 2'-deoxyribonucleoside triphosphates (dNTPs) for both replication and repair of damaged DNA predominantly through de novo reduction of intracellular ribonucleotides by ribonucleotide reductase (RNR). Cells can also salvage deoxynucleosides by d... |
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Modulating radiation resistance by inhibiting ribonucleotide reductase in cancers with virally or mutationally silenced p53 protein.
Radiat. Res. 172(6) , 666-76, (2009) Therapeutic ionizing radiation damages DNA, increasing p53-regulated ribonucleotide reductase (RNR) activity required for de novo synthesis of the deoxyribonucleotide triphosphates used during DNA repair. This study investigated the pharmacological inhibition... |
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Radiosensitization of human cervical cancer cells by inhibiting ribonucleotide reductase: enhanced radiation response at low-dose rates.
Int. J. Radiat. Oncol. Biol. Phys. 80(4) , 1198-204, (2011) To test whether pharmacologic inhibition of ribonucleotide reductase (RNR) by 3-aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP, NSC #663249) enhances radiation sensitivity during low-dose-rate ionizing radiation provided by a novel purpose-built iridi... |
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Ribonucleotide reductase inhibition restores platinum-sensitivity in platinum-resistant ovarian cancer: a Gynecologic Oncology Group Study.
J. Transl. Med. 10 , 79, (2012) The potent ribonucleotide reductase (RNR) inhibitor 3-aminopyridine-2-carboxyaldehyde-thiosemicarbazone (3-AP) was tested as a chemosensitizer for restored cisplatin-mediated cytotoxicity in platinum-resistant ovarian cancer.Preclinical in vitro platinum-resi... |
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A dose escalation and pharmacodynamic study of triapine and radiation in patients with locally advanced pancreas cancer.
Int. J. Radiat. Oncol. Biol. Phys. 84(4) , e475-81, (2012) Triapine, a novel inhibitor of the M2 subunit of ribonucleotide reductase (RR), is a potent radiosensitizer. This phase 1 study, sponsored by the National Cancer Institute Cancer Therapy Evaluation Program, assessed the safety and tolerability of triapine in ... |
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Aryl- and heteroaryl-thiosemicarbazone derivatives and their metal complexes: a pharmacological template.
Recent Pat. Anticancer. Drug Discov. 8(2) , 168-82, (2013) In this review, we discuss the current patents concerning aryl/heteroaryl thiosemicarbazone derivatives as regards to their activities and properties, including coordination (chelation) properties. The mode of action of the aryl/heteroaryl thiosemicarbazone d... |