Amsacrine
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| Amsacrine
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| Systematic (IUPAC) name | |
| N-(4-(acridin-9-ylamino)-3-methoxyphenyl)methanesulfonamide | |
| Identifiers | |
| CAS number | |
| ATC code | L01 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C21H19N3O3S |
| Mol. mass | 393.46 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | 96 to 98% |
| Metabolism | ? |
| Half life | 8-9 hours |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
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| Routes | ? |
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Overview
Amsacrine is an antineoplastic agent. Its planar fused ring system can intercalate into the DNA of tumor cells, thereby altering the major and minor groove proportions. These alterations to DNA structure inhibit both DNA replication and transcription by reducing association between the affected DNA and: DNA polymerase, RNA polymerase and transcription factors.
Amsacrine also expresses topoisomerase inhibitor activity, specifically inhibiting topoisomerase II (compares with the better known agent etoposide).[1]
References
- ↑ Genetic Response to Metals. Sarkar, Bibudhendra. CRC Press, 1995. ISBN 9780824796150
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